NAMPT inhibitors

ABSTRACT

Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed.

This application claims priority to Patent Cooperation Treaty PatentApplication Serial No. PCT/CN2012/075327, filed May 11, 2012, which isincorporated by reference in their entirety.

FIELD OF THE INVENTION

This invention pertains to compounds which inhibit the activity ofNAMPT, compositions containing the compounds, and methods of treatingdiseases during which NAMPT is expressed.

BACKGROUND OF THE INVENTION

NAD+ (nicotinamide adenine dinucleotide) is a coenzyme that plays acritical role in many physiologically essential processes (Ziegkel, M.Eur. J. Biochem. 267, 1550-1564, 2000). NAD is necessary for severalsignaling pathways including among others poly ADP-ribosylation in DNArepair, mono-ADP-ribosylation in both the immune system andG-protein-coupled signaling, and NAD is also required by sirtuins fortheir deacetylase activity (Garten, A. et al Trends in Endocrinology andMetabolism, 20, 130-138, 2008).

NAMPT (also known as pre-B-cell-colony-enhancing factor (PBEF) andvisfatin) is an enzyme that catalyzes the phosphoribosylation ofnicotinamide and is the rate-limiting enzyme in one of two pathways thatsalvage NAD.

Increasing evidence suggests that NAMPT inhibitors have potential asanticancer agents. Cancer cells have a higher basal turnover of NAD andalso display higher energy requirements compared with normal cells.Additionally, increased NAMPT expression has been reported in colorectalcancer (Van Beijnum, J. R. et al Int. J. Cancer 101, 118-127, 2002) andNAMPT is involved in angiogenesis (Kim, S. R. et al. Biochem. Biophys.Res. Commun. 357, 150-156, 2007). Small-molecule inhibitors of NAMPThave been shown to cause depletion of intracellular NAD+ levels andultimately induce tumor cell death (Hansen, C M et al. Anticancer Res.20, 42111-4220, 2000) as well as inhibit tumor growth in xenograftmodels (Olese, U. H. et al. Mol Cancer Ther. 9, 1609-1617, 2010).

NAMPT inhibitors also have potential as therapeutic agents ininflammatory and metabolic disorders (Galli, M. et al Cancer Res. 70,8-11, 2010). For example, NAMPT is the predominant enzyme in T and Blymphocytes. Selective inhibition of NAMPT leads to NAD+ depletion inlymphocytes blocking the expansion that accompanies autoimmune diseaseprogression whereas cell types expressing the other NAD+ generatingpathways might be spared. A small molecule NAMPT inhibitor (FK866) hasbeen shown to selectively block proliferation and induce apoptosis ofactivated T cells and was efficacious in animal models of arthritis(collagen-induced arthritis) (Busso, N. et al. Plos One 3, e2267, 2008).FK866 ameliorated the manifestations of experimental autoimmuneencephalomyelitis (EAE), a model of T-cell mediated autoimmunedisorders. (Bruzzone, S et al. Plos One 4, e7897, 2009). NaMPT activityincreases NF-kB transcriptional activity in human vascular endothelialcell, resulting in MMP-2 and MMP-9 activation, suggesting a role forNAMPT inhibitors in the prevention of inflammatory mediatedcomplications of obesity and type 2 diabetes (Adya, R. et. Al. DiabetesCare, 31, 758-760, 2008).

SUMMARY OF THE INVENTION

One embodiment of this invention, therefore, pertains to compounds orpharmaceutically acceptable salts thereof, which are useful asinhibitors of NAMPT, the compounds having Formula (I)

wherein

R¹ and R² are each independently selected from the group consisting ofR⁶, C(O)R⁶, C(O)NHR⁶, and C(O)N(R⁶)₂; wherein at least one of R¹ and R²is R⁶; or

R¹ and R², together with the nitrogen to which they are attached form aheterocycloalkyl or heterocycloalkenyl ring; wherein the ring formedwith R¹ and R² together with the nitrogen to which they are attached isoptionally substituted with one or more substituents independentlyselected from the group consisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷,C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷,NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂,NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷,C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂,SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R³, R⁴, and R⁵ are each independently selected from the group consistingof hydrogen, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl,C₁₋₆ hydroxyalkyl, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁶ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR⁸, OR⁸, SR⁸, S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂,NHR⁸, N(R⁸)₂, NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸,NR⁸C(O)OR⁸, NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸,NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸,C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein the aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl represented by R⁶ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁷ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofaryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁷ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁸ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰,OC(O)OR¹⁰, NH₂, NHR¹⁰, N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰,NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰, NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰,NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰, NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰,C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰, C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂,SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂,CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁸ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹, C(O)R¹¹,CO(O)R¹¹, OC(O)R¹¹, OC(O)OR¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹,NR¹¹C(O)R¹¹, NHS(O)₂R¹¹, NR¹¹S(O)₂R¹¹, NHC(O)OR¹¹, NR¹¹C(O)OR¹¹,NHC(O)NH₂, NHC(O)NHR¹¹, NHC(O)N(R¹¹)₂, NR¹¹C(O)NHR¹¹, NR¹¹C(O)N(R¹¹)₂,C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)NHOH, C(O)NHOR¹¹, C(O)NHSO₂R¹¹,C(O)NR¹¹SO₂R¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹¹, C(N)N(R¹¹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁹, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁹ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹², OR¹², SR¹², S(O)R¹², SO₂R¹², C(O)R¹², CO(O)R¹², OC(O)R¹²,OC(O)OR¹², NH₂, NHR¹², N(R¹²)₂, NHC(O)R¹², NR¹²C(O)R¹², NHS(O)₂R¹²,NR¹²S(O)₂R¹², NHC(O)OR¹², NR¹²C(O)OR¹², NHC(O)NH₂, NHC(O)NHR¹²,NHC(O)N(R¹²)₂, NR¹²C(O)NHR¹², NR¹²C(O)N(R¹²)₂, C(O)NH₂, C(O)NHR¹²,C(O)N(R¹²)₂, C(O)NHOH, C(O)NHOR¹², C(O)NHSO₂R¹², C(O)NR¹²SO₂R¹², SO₂NH₂,SO₂NHR¹², SO₂N(R¹²)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR¹², C(N)N(R¹²)₂,CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁹ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³,CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³,NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³,NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂,C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³,C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹³, C(N)N(R¹³)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl,and C₁₋₆ hydroxyalkyl;

R¹¹, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R¹¹ are each independently optionally substituted withone or more substituents independently selected from the groupconsisting of C₁₋₆ alkoxy, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I; wherein the aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl representedby R¹¹ are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of NH₂,C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;

R¹², at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R¹² are each independently optionally substituted withone or more substituents independently selected from the groupconsisting of C₁₋₆ alkoxy, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I; wherein the aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl representedby R¹² are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of NH₂,C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I; and

R¹³, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl; wherein theC₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl represented by R¹³ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of alkoxy, NH₂, C(O)H,C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I.

In one embodiment of Formula (I), R¹ is C(O)R⁶; and R² is R⁶. In anotherembodiment of Formula (I), R¹ and R² are each R⁶. In another embodimentof Formula (I), R¹ is C(O)NHR⁶; and R² is R⁶. In another embodiment ofFormula (I), R¹ is C(O)N(R⁶)₂; and R² is R⁶. In another embodiment ofFormula (I), R³, R⁴ and R⁵ are hydrogen. In another embodiment ofFormula (I), R⁶, at each occurrence, is independently selected from thegroup consisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, aryl, heterocycloalkyl,heteroaryl, and cycloalkyl; wherein the C₁₋₆ alkyl, and C₂₋₆ alkenylrepresented by R⁶ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR⁸, OR⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, N(R⁸)₂, NHC(O)R⁸, C(O)NH₂, C(O)NHR⁸,C(O)N(R⁸)₂, C(O)OH, and OH; wherein the aryl, heterocycloalkyl,heteroaryl, and cycloalkyl represented by R⁶ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R⁹, OR⁹, C(O)NH₂, C(O)OH, OH, CN,F, Cl, Br and I.

Still another embodiment pertains to compounds, which are

-   2-{(4-fluorobenzyl)[4-(pyridin-3-yl)benzyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{methyl[4-(pyridin-3-yl)benzyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(methyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(tetrahydro-2H-pyran-4-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(cyclohexylacetyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(3-methylbutanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[3-(morpholin-4-yl)propyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[3-(piperidin-1-yl)propyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[2-(pyrrolidin-1-yl)ethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){2-[4-(propan-2-yl)piperazin-1-yl]ethyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzoyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(3-chlorobenzoyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzoyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(5-chloro-1,3-benzodioxol-4-yl)methyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-chlorobenzyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(2-chlorobenzyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(2,5-dichlorobenzyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[2-(methylamino)-2-oxoethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[2-oxo-2-(propan-2-ylamino)ethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(dimethylamino)-2-oxoethyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(diethylamino)-2-oxoethyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[2-(morpholin-4-yl)-2-oxoethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(4-methylbenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(methoxyacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(N,N-dimethylglycyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(3,6-dihydropyridin-1(2H)-ylacetyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(4-methylpiperidin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(4-hydroxypiperidin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(4-methylpiperazin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[4-(propan-2-yl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(4-formylpiperazin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(hexahydropyrrolo[1,2-a]pyrazin-2(1H)-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[4-(cyclopropylmethyl)piperazin-1-yl]acetyl}(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[4-(2-ethoxyethyl)piperazin-1-yl]acetyl}(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(cyclopropylcarbonyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[4-(prop-2-en-1-yl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[4-(3-methoxypropyl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[3-(dimethylamino)pyrrolidin-1-yl]acetyl}(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(morpholin-4-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(3-hydroxypiperidin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[4-(2-hydroxyethyl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(1,4-dioxa-7-azaspiro[4.4]non-7-ylacetyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   1-{2-[(4-fluorobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)amino]-2-oxoethyl}pyridinium;-   2-{[2-(4-fluorophenyl)ethyl](3-methylbutanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(propan-2-ylcarbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(4-cyanophenyl)ethyl](3-methylbutanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(4-cyanophenyl)ethyl](tetrahydro-2H-pyran-4-ylacetyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methylbutanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(tetrahydro-2H-pyran-4-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(4-cyanophenyl)ethyl](tetrahydrofuran-3-ylacetyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(3-methylbutanoyl)amino]-N-[3-(2-methyl-1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(3-methylbutanoyl)amino]-N-[3-(4-methyl-1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(2-fluorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(3-fluorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(2-chlorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(3-chlorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-chlorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(tetrahydrofuran-3-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(3-methylbutyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-methylpropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N¹-(4-fluorobenzyl)-N¹-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)piperidine-1,3-dicarboxamide;-   2-{(4-fluorobenzyl)[(3-hydroxyazetidin-1-yl)carbonyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-1,4-dioxa-7-azaspiro[4.4]nonane-7-carboxamide;-   2-{(4-fluorobenzyl)[(3-methoxypyrrolidin-1-yl)carbonyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-methoxyethyl)(methyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-2,6-dimethylmorpholine-4-carboxamide;-   2-{[ethyl(2-methoxyethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-2,2-dimethylmorpholine-4-carboxamide;-   N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-1,4-oxazepane-4-carboxamide;-   2-[(4-fluorobenzoyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(4-methylbenzyl)amino]-1,3-thiazole-5-carboxamide;-   N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-N-(3-methylbutyl)-1,2-oxazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(2-phenoxypropanoyl)amino]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-propoxyethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(tetrahydrofuran-2-ylmethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(1-methoxypropan-2-yl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-methoxyethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(2-ethoxyethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(1-methoxybutan-2-yl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(4-cyanophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(1,3-dioxolan-2-ylmethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[2-(propan-2-yloxy)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(1,4-dioxan-2-ylmethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(1,3-dimethoxypropan-2-yl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-methoxybutyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(tetrahydrofuran-3-ylcarbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(tetrahydro-2H-pyran-3-ylcarbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(pyrimidin-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(2-methoxypyridin-4-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(1,3-oxazol-4-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   2-{[(5-chloropyridin-2-yl)methyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(4-methylpyridin-3-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(6-methoxypyridin-3-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(4-methyl-1,3-thiazol-5-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[2-(3-hydroxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(pyridin-2-yl)ethyl]amino}-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(1,3-benzodioxol-5-yl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(4-chlorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(3-fluorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(4-hydroxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(3-chlorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   N-[3-(1H-imidazol-1-yl)propyl]-2-{[2-(3-methoxyphenyl)ethyl](3-methoxypropanoyl)amino}-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(2-fluorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-hydroxy-2-(4-methoxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[1-(pyridin-2-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(1-methyl-1H-pyrazol-4-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(2,6-difluorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(6-methylpyridin-3-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(4-chlorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(5-methylpyrazin-2-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(3-chlorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(5-methylpyridin-2-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(2,5-difluorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(2-methylbenzyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(3-methylbenzyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(pyridin-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(pyridin-3-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[2-(propan-2-yloxy)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(2-methoxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[2-(2-hydroxyethoxy)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(propan-2-yloxy)propyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(3-hydroxy-2,2-dimethylpropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(2-hydroxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(1-hydroxypropan-2-yl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(3-hydroxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[(2S)-1-hydroxybut-3-en-2-yl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(4-hydroxybutyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methylbutyl)[(2R)-2-phenoxypropanoyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methylbutyl)[(2S)-2-phenoxypropanoyl]amino}-1,3-thiazole-5-carboxamide;-   N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-5-methyl-N-(3-methylbutyl)-1,2-oxazole-3-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(phenoxyacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(3-phenylpropanoyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(2-phenylpropanoyl)amino]-1,3-thiazole-5-carboxamide;-   2-{[(4-fluorophenyl)acetyl](3-methylbutyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(3-amino-3-oxopropyl)carbamoyl](4-cyanobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[3-(acetylamino)-2-methylpropyl]carbamoyl}(4-cyanobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(dimethylamino)-3-oxopropyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(3-ethoxy-2-hydroxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(diethylamino)propyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[2-(acetylamino)ethyl]carbamoyl}(4-cyanobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[2-(diethylamino)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)({2-[(2-methylpropanoyl)amino]ethyl}carbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[(2R)-1-hydroxybut-3-en-2-yl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(3-hydroxyazetidin-1-yl)propyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(3-methylbutyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(methoxyacetyl)(3-methylbutyl)amino]-1,3-thiazole-5-carboxamide;-   2-[(cyclopropylcarbonyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   (2S)-1-[(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-athiazol-2-yl)(3-methylbutyl)amino]-1-oxopropan-2-yl    acetate;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydro-2H-pyran-4-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydrofuran-3-ylcarbonyl)amino]-1,3-thiazole-5-carboxamide;-   2-{[2-hydroxy-2-(3-methoxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(pyrazin-2-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[1-(3-hydroxyphenyl)propan-2-yl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   ethyl    N-[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]-beta-alaninate;-   ethyl    4-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoate;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoate;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-4-methylpentanoate;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2,2-dimethylpropanoate;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}cyclobutanecarboxylic    acid;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2-methylpropanoate;-   2-{(4-cyanobenzyl)[(3-methoxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoic    acid;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-4-methylpentanoic    acid;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2,2-dimethylpropanoic    acid;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2-methylpropanoic    acid;-   N-[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]-beta-alanine;-   4-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoic    acid;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydrofuran-2-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydrofuran-3-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(3-methoxypropanoyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(3-methoxypropyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(tetrahydro-2H-pyran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(tetrahydrofuran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(propan-2-yloxy)ethyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[2-(1,3-dioxolan-2-yl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(1,4-dioxan-2-ylmethyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[3-(4-fluorophenyl)propanoyl](2-methoxyethyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(2-methoxyethyl)[3-(pyridin-3-yl)propanoyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(pyridin-3-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(2-methoxyethyl)(naphthalen-2-ylacetyl)amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(2-methoxyethyl)[(4-phenoxyphenyl)acetyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[(4-cyanophenyl)acetyl](2-methoxyethyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(4-aminophenyl)acetyl](2-methoxyethyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{2-[di(prop-2-en-1-yl)amino]ethyl}(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[3-(diethylamino)propyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(diethylamino)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-(pyrrolidin-1-yl)propyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[(1-ethyl-5-oxopyrrolidin-3-yl)methyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(5-oxopyrrolidin-2-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-oxo-3-(pyrrolidin-1-yl)propyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-oxo-2-(piperidin-1-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-(2-oxopyrrolidin-1-yl)propyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(2-oxo-1,3-oxazolidin-3-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl){2-[(2-methylpropanoyl)amino]ethyl}amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-(methylamino)-3-oxopropyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[3-(acetylamino)propyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-oxo-2-(pyrrolidin-1-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   2-[3-(2-hydroxyethyl)-2-oxoimidazolidin-1-yl]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[3-(4-fluorophenyl)-2-oxoimidazolidin-1-yl]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(5-chloropyridin-2-yl)methyl](tetrahydro-2H-pyran-4-ylcarbonyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(5-chloropyridin-2-yl)methyl](tetrahydrofuran-3-ylcarbonyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(5-chloropyridin-2-yl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(5-chloropyridin-2-yl)ethyl](tetrahydro    furan-3-ylcarbonyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(5-chloropyridin-2-yl)ethyl][(2-methoxyethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-([2-(5-chloropyridin-2-yl)ethyl]{[2-(propan-2-yloxy)ethyl]carbamoyl}amino)-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(1,3-benzodioxol-5-ylacetyl)(2-methoxyethyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(5S)-5-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-2-oxo-1,3-oxazolidin-3-yl}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(pyridin-2-ylacetyl)amino]-1,3-thiazole-5-carboxamide;    and pharmaceutically acceptable salts thereof.

Another embodiment pertains to a composition for treating inflammatoryand tissue repair disorders; particularly rheumatoid arthritis,inflammatory bowel disease, asthma and COPD (chronic obstructivepulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases;dermatosis, including psoriasis, atopic dermatitis and ultra-violetinduced skin damage; autoimmune diseases including systemic upuserythematosis, multiple sclerosis, psoriatic arthritis, ankylosingspondylitis, tissue and organ rejection, Alzheimer's disease, stroke,athersclerosis, restenosis, diabetes, glomerulonephritis, cancer,particularly wherein the cancer is selected from breast, prostate, lung,colon, cervix, ovary, skin, CNS, bladder, pancreas, leukemia, lymphomaor Hodgkin's disease, cachexia, inflammation associated with infectionand certain viral infections, including Acquired Immune DeficiencySyndrome (AIDS), adult respiratory distress syndrome, and ataxiatelengiectasia, said composition comprising an excipient and atherapeutically effective amount of a compound of Formula (I), orpharmaceutically acceptable salts thereof.

Another embodiment pertains to a method of treating inflammatory andtissue repair disorders; particularly rheumatoid arthritis, inflammatorybowel disease, asthma and COPD (chronic obstructive pulmonary disease),osteoarthritis, osteoporosis and fibrotic diseases; dermatosis,including psoriasis, atopic dermatitis and ultra-violet induced skindamage; autoimmune diseases including systemic lupus erythematosis,multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissueand organ rejection, Alzheimer's disease, stroke, athersclerosis,restenosis, diabetes, glomerulonephritis, cancer, particularly whereinthe cancer is selected from breast, prostate, lung, colon, cervix,ovary, skin, CNS, bladder, pancreas, leukemia, lymphoma or Hodgkin'sdisease, cachexia, inflammation associated with infection and certainviral infections, including Acquired Immune Deficiency Syndrome (AIDS),adult respiratory distress syndrome, and ataxia telengiectasia in apatient, said method comprising administering to the patient atherapeutically effective amount of a compound of Formula (I), orpharmaceutically acceptable salts thereof.

Another embodiment pertains to a method of treating inflammatory andtissue repair disorders; particularly rheumatoid arthritis, inflammatorybowel disease, asthma and COPD (chronic obstructive pulmonary disease),osteoarthritis, osteoporosis and fibrotic diseases; dermatosis,including psoriasis, atopic dermatitis and ultra-violet induced skindamage; autoimmune diseases including systemic lupus erythematosis,multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissueand organ rejection, Alzheimer's disease, stroke, athersclerosis,restenosis, diabetes, glomerulonephritis, cancer, particularly whereinthe cancer is selected from breast, prostate, lung, colon, cervix,ovary, skin, CNS, bladder, pancreas, leukemia, lymphoma or Hodgkin'sdisease, cachexia, inflammation associated with infection and certainviral infections, including Acquired Immune Deficiency Syndrome (AIDS),adult respiratory distress syndrome, and ataxia telengiectasia or spleencancer in a patient, said method comprising administering to the patienttherapeutically effective amount of the compound of Formula (I), orpharmaceutically acceptable salts thereof; and a therapeuticallyeffective amount of one additional therapeutic agent or more than oneadditional therapeutic agent.

DETAILED DESCRIPTION OF THE INVENTION

This detailed description is intended only to acquaint others skilled inthe art with Applicants' invention, its principles, and its practicalapplication so that others skilled in the art may adapt and apply theinvention in its numerous forms, as they may be best suited to therequirements of a particular use. This description and its specificexamples are intended for purposes of illustration only. This invention,therefore, is not limited to the embodiments described in this patentapplication, and may be variously modified.

Abbreviations and Definitions

Unless otherwise defined herein, scientific and technical terms used inconnection with the present invention shall have the meanings that arecommonly understood by those of ordinary skill in the art. The meaningand scope of the terms should be clear, however, in the event of anylatent ambiguity, definitions provided herein take precedent over anydictionary or extrinsic definition. In this application, the use of “or”means “and/or” unless stated otherwise. Furthermore, the use of the term“including”, as well as other forms, such as “includes” and “included”,is not limiting. With reference to the use of the words “comprise” or“comprises” or “comprising” in this patent application (including theclaims), Applicants note that unless the context requires otherwise,those words are used on the basis and clear understanding that they areto be interpreted inclusively, rather than exclusively, and thatApplicants intend each of those words to be so interpreted in construingthis patent application, including the claims below. For a variable thatoccurs more than one time in any substituent or in the compound of theinvention or any other formulae herein, its definition on eachoccurrence is independent of its definition at every other occurrence.Combinations of substituents are permissible only if such combinationsresult in stable compounds. Stable compounds are compounds which can beisolated in a useful degree of purity from a reaction mixture.

It is meant to be understood that proper valences are maintained for allcombinations herein, that monovalent moieties having more than one atomare attached through their left ends, and that divalent moieties aredrawn from left to right.

As used in the specification and the appended claims, unless specifiedto the contrary, the following terms have the meaning indicated:

The term “alkyl” (alone or in combination with another term(s)) means astraight- or branched-chain saturated hydrocarbyl substituent typicallycontaining from 1 to about 10 carbon atoms; or in another embodiment,from 1 to about 8 carbon atoms; in another embodiment, from 1 to about 6carbon atoms; and in another embodiment, from 1 to about 4 carbon atoms.Examples of such substituents include methyl, ethyl, n-propyl,isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, pentyl, iso-amyl,and hexyl and the like.

The term “alkenyl” (alone or in combination with another term(s)) meansa straight- or branched-chain hydrocarbyl substituent containing one ormore double bonds and typically from 2 to about 10 carbon atoms; or inanother embodiment, from 2 to about 8 carbon atoms; in anotherembodiment, from 2 to about 6 carbon atoms; and in another embodiment,from 2 to about 4 carbon atoms. Examples of such substituents includeethenyl (vinyl), 2-propenyl, 3-propenyl, 1,4-pentadienyl,1,4-butadienyl, 1-butenyl, 2-butenyl, and 3-butenyl and the like.

The term “alkynyl” (alone or in combination with another term(s)) meansa straight- or branched-chain hydrocarbyl substituent containing one ormore triple bonds and typically from 2 to about 10 carbon atoms; or inanother embodiment, from 2 to about 8 carbon atoms; in anotherembodiment, from 2 to about 6 carbon atoms; and in another embodiment,from 2 to about 4 carbon atoms. Examples of such substituents includeethynyl, 2-propynyl, 3-propynyl, 2-butynyl, and 3-butynyl and the like.

The term “carbocyclyl” (alone or in combination with another term(s))means a saturated cyclic (i.e., “cycloalkyl”), partially saturatedcyclic (i.e., “cycloalkenyl”), or completely unsaturated (i.e., “aryl”)hydrocarbyl substituent containing from 3 to 14 carbon ring atoms (“ringatoms” are the atoms bound together to form the ring or rings of acyclic substituent). A carbocyclyl may be a single-ring (monocyclic) orpolycyclic ring structure.

A carbocyclyl may be a single ring structure, which typically containsfrom 3 to 8 ring atoms, more typically from 3 to 6 ring atoms, and evenmore typically 5 to 6 ring atoms. Examples of such single-ringcarbocyclyls include cyclopropyl (cyclopropanyl), cyclobutyl(cyclobutanyl), cyclopentyl (cyclopentanyl), cyclopentenyl,cyclopentadienyl, cyclohexyl (cyclohexanyl), cyclohexenyl,cyclohexadienyl, and phenyl. A carbocyclyl may alternatively bepolycyclic (i.e., may contain more than one ring). Examples ofpolycyclic carbocyclyls include bridged, fused, and spirocycliccarbocyclyls. In a spirocyclic carbocyclyl, one atom is common to twodifferent rings. An example of a spirocyclic carbocyclyl isspiropentanyl. In a bridged carbocyclyl, the rings share at least twocommon non-adjacent atoms. Examples of bridged carbocyclyls includebicyclo[2.2.1]heptanyl, bicyclo[2.2.1]hept-2-enyl, and adamantanyl. In afused-ring carbocyclyl system, two or more rings may be fused together,such that two rings share one common bond. Examples of two- orthree-fused ring carbocyclyls include naphthalenyl,tetrahydronaphthalenyl (tetralinyl), indenyl, indanyl (dihydroindenyl),anthracenyl, phenanthrenyl, and decalinyl.

The term “cycloalkyl” (alone or in combination with another term(s))means a saturated cyclic hydrocarbyl substituent containing from 3 to 14carbon ring atoms. A cycloalkyl may be a single carbon ring, whichtypically contains from 3 to 8 carbon ring atoms and more typically from3 to 6 ring atoms. Examples of single-ring cycloalkyls includecyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl. A cycloalkyl mayalternatively be polycyclic or contain more than one ring. Examples ofpolycyclic cycloalkyls include bridged, fused, and spirocycliccarbocyclyls.

The term “aryl” (alone or in combination with another term(s)) means anaromatic carbocyclyl containing from 6 to 14 carbon ring atoms. An arylmay be monocyclic or polycyclic (i.e., may contain more than one ring).In the case of polycyclic aromatic rings, only one ring the polycyclicsystem is required to be unsaturated while the remaining ring(s) may besaturated, partially saturated or unsaturated. Examples of aryls includephenyl, naphthalenyl, indenyl, indanyl, and tetrahydronapthyl.

In some instances, the number of carbon atoms in a hydrocarbylsubstituent (e.g., alkyl, alkenyl, alkynyl, or cycloalkyl) is indicatedby the prefix “C_(x)-C_(y)-”, wherein x is the minimum and y is themaximum number of carbon atoms in the substituent. Thus, for example,“C₁-C₆-alkyl” refers to an alkyl substituent containing from 1 to 6carbon atoms. Illustrating further, C₃-C₈-cycloalkyl means a saturatedhydrocarbyl ring containing from 3 to 8 carbon ring atoms.

The term “hydrogen” (alone or in combination with another term(s)) meansa hydrogen radical, and may be depicted as —H.

The term “hydroxy” (alone or in combination with another term(s)) means—OH.

The term “carboxy” (alone or in combination with another term(s)) means—C(O)—OH.

The term “amino” (alone or in combination with another term(s)) means—NH₂.

The term “halogen” or “halo” (alone or in combination with anotherterm(s)) means a fluorine radical (which may be depicted as —F),chlorine radical (which may be depicted as —Cl), bromine radical (whichmay be depicted as —Br), or iodine radical (which may be depicted as—I).

If a substituent is described as being “substituted”, a non-hydrogenradical is in the place of hydrogen radical on a carbon or nitrogen ofthe substituent. Thus, for example, a substituted alkyl substituent isan alkyl substituent in which at least one non-hydrogen radical is inthe place of a hydrogen radical on the alkyl substituent. To illustrate,monofluoroalkyl is alkyl substituted with a fluoro radical, anddifluoroalkyl is alkyl substituted with two fluoro radicals. It shouldbe recognized that if there are more than one substitution on asubstituent, each non-hydrogen radical may be identical or different(unless otherwise stated).

If a substituent is described as being “optionally substituted”, thesubstituent may be either (1) not substituted or (2) substituted. If asubstituent is described as being optionally substituted with up to aparticular number of non-hydrogen radicals, that substituent may beeither (1) not substituted; or (2) substituted by up to that particularnumber of non-hydrogen radicals or by up to the maximum number ofsubstitutable positions on the substituent, whichever is less. Thus, forexample, if a substituent is described as a heteroaryl optionallysubstituted with up to 3 non-hydrogen radicals, then any heteroaryl withless than 3 substitutable positions would be optionally substituted byup to only as many non-hydrogen radicals as the heteroaryl hassubstitutable positions. To illustrate, tetrazolyl (which has only onesubstitutable position) would be optionally substituted with up to onenon-hydrogen radical. To illustrate further, if an amino nitrogen isdescribed as being optionally substituted with up to 2 non-hydrogenradicals, then a primary amino nitrogen will be optionally substitutedwith up to 2 non-hydrogen radicals, whereas a secondary amino nitrogenwill be optionally substituted with up to only 1 non-hydrogen radical.

This patent application uses the terms “substituent” and “radical”interchangeably.

The prefix “halo” indicates that the substituent to which the prefix isattached is substituted with one or more independently selected halogenradicals. For example, haloalkyl means an alkyl substituent in which atleast one hydrogen radical is replaced with a halogen radical. Examplesof haloalkyls include chloromethyl, 1-bromoethyl, fluoromethyl,difluoromethyl, trifluoromethyl, and 1,1,1-trifluoroethyl. It should berecognized that if a substituent is substituted by more than one halogenradical, those halogen radicals may be identical or different (unlessotherwise stated).

The prefix “perhalo” indicates that every hydrogen radical on thesubstituent to which the prefix is attached is replaced withindependently selected halogen radicals, i.e., each hydrogen radical onthe substituent is replaced with a halogen radical. If all the halogenradicals are identical, the prefix typically will identify the halogenradical. Thus, for example, the term “perfluoro” means that everyhydrogen radical on the substituent to which the prefix is attached issubstituted with a fluorine radical. To illustrate, the term“perfluoroalkyl” means an alkyl substituent wherein a fluorine radicalis in the place of each hydrogen radical.

The term “carbonyl” (alone or in combination with another term(s)) means—C(O)—.

The term “aminocarbonyl” (alone or in combination with another term(s))means —C(O)—NH₂.

The term “oxo” (alone or in combination with another term(s)) means(═O).

The term “oxy” (alone or in combination with another term(s)) means anether substituent, and may be depicted as —O—.

The term “alkylhydroxy” (alone or in combination with another term(s))means alkyl-OH.

The term “alkylamino” (alone or in combination with another term(s))means alkyl-NH₂.

The term “alkyloxy” (alone or in combination with another term(s)) meansan alkylether substituent, i.e., —O-alkyl. Examples of such asubstituent include methoxy (—O—CH₃), ethoxy, n-propoxy, isopropoxy,n-butoxy, iso-butoxy, sec-butoxy, and tert-butoxy.

The term “alkylcarbonyl” (alone or in combination with another term(s))means —C(O)-alkyl.

The term “aminoalkylcarbonyl” (alone or in combination with anotherterm(s)) means —C(O)-alkyl-NH₂.

The term “alkyloxycarbonyl” (alone or in combination with anotherterm(s)) means —C(O)—O-alkyl.

The term “carbocyclylcarbonyl” (alone or in combination with anotherterm(s)) means —C(O)-carbocyclyl.

Similarly, the term “heterocyclylcarbonyl” (alone or in combination withanother term(s)) means —C(O)-heterocyclyl.

The term “carbocyclylalkylcarbonyl” (alone or in combination withanother term(s)) means —C(O)-alkyl-carbocyclyl.

Similarly, the term “heterocyclylalkylcarbonyl” (alone or in combinationwith another term(s)) means —C(O)-alkyl-heterocyclyl.

The term “carbocyclyloxycarbonyl” (alone or in combination with anotherterm(s)) means —C(O)—O-carbocyclyl.

The term “carbocyclylalkyloxycarbonyl” (alone or in combination withanother term(s)) means —C(O)—O-alkyl-carbocyclyl.

The term “thio” or “thia” (alone or in combination with another term(s))means a thiaether substituent, i.e., an ether substituent wherein adivalent sulfur atom is in the place of the ether oxygen atom. Such asubstituent may be depicted as —S—. This, for example,“alkyl-thio-alkyl” means alkyl-S-alkyl (alkyl-sulfanyl-alkyl).

The term “thiol” or “sulfhydryl” (alone or in combination with anotherterm(s)) means a sulfhydryl substituent, and may be depicted as —SH.

The term “(thiocarbonyl)” (alone or in combination with another term(s))means a carbonyl wherein the oxygen atom has been replaced with asulfur. Such a substituent may be depicted as —C(S)—.

The term “sulfonyl” (alone or in combination with another term(s)) means—S(O)₂—.

The term “aminosulfonyl” (alone or in combination with another term(s))means —S(O)₂—NH₂.

The term “sulfinyl” or “sulfoxido” (alone or in combination with anotherterm(s)) means —S(O)—.

The term “heterocyclyl” (alone or in combination with another term(s))means a saturated (i.e., “heterocycloalkyl”), partially saturated (i.e.,“heterocycloalkenyl”), or completely unsaturated (i.e., “heteroaryl”)ring structure containing a total of 3 to 14 ring atoms. At least one ofthe ring atoms is a heteroatom (i.e., oxygen, nitrogen, or sulfur), withthe remaining ring atoms being independently selected from the groupconsisting of carbon, oxygen, nitrogen, and sulfur. A heterocyclyl maybe a single-ring (monocyclic) or polycyclic ring structure.

A heterocyclyl may be a single ring, which typically contains from 3 to7 ring atoms, more typically from 3 to 6 ring atoms, and even moretypically 5 to 6 ring atoms. Examples of single-ring heterocyclylsinclude 1,2,3,6-tetrahydropyridine, thiomorpholinyl, tetrahydropyranyl,furanyl, dihydrofuranyl, tetrahydrofuranyl, thiophenyl (thiofuranyl),dihydrothiophenyl, tetrahydrothiophenyl, pyrrolyl, pyrrolinyl,pyrrolidinyl, imidazolyl, imidazolinyl, imidazolidinyl, pyrazolyl,pyrazolinyl, pyrazolidinyl, triazolyl, tetrazolyl, oxazolyl,oxazolidinyl, isoxazolidinyl, isoxazolyl, thiazolyl, isothiazolyl,thiazolinyl, isothiazolinyl, thiazolidinyl, isothiazolidinyl,thiodiazolyl, oxadiazolyl (including 1,2,3-oxadiazolyl,1,2,4-oxadiazolyl, 1,2,5-oxadiazolyl (furazanyl), or 1,3,4-oxadiazolyl),oxatriazolyl (including 1,2,3,4-oxatriazolyl or 1,2,3,5-oxatriazolyl),dioxazolyl (including 1,2,3-dioxazolyl, 1,2,4-dioxazolyl,1,3,2-dioxazolyl, or 1,3,4-dioxazolyl), oxathiazolyl, oxathiolyl,oxathiolanyl, pyranyl, dihydropyranyl, thiopyranyl,tetrahydrothiopyranyl, pyridinyl (azinyl), piperidinyl, diazinyl(including pyridazinyl (1,2-diazinyl), pyrimidinyl (1,3-diazinyl), orpyrazinyl (1,4-diazinyl)), piperazinyl, pyrrolidin-2-only, triazinyl(including 1,3,5-triazinyl, 1,2,4-triazinyl, and 1,2,3-triazinyl)),oxazinyl (including 1,2-oxazinyl, 1,3-oxazinyl, or 1,4-oxazinyl)),oxathiazinyl (including 1,2,3-oxathiazinyl, 1,2,4-oxathiazinyl,1,2,5-oxathiazinyl, or 1,2,6-oxathiazinyl)), oxadiazinyl (including1,2,3-oxadiazinyl, 1,2,4-oxadiazinyl, 1,4,2-oxadiazinyl, or1,3,5-oxadiazinyl)), morpholinyl, azepinyl, oxepinyl, thiepinyl, anddiazepinyl.

A heterocyclyl may alternatively be polycyclic (i.e., may contain morethan one ring). Examples of polycyclic heterocyclyls include bridged,fused, and spirocyclic heterocyclyls. In a spirocyclic heterocyclyl, oneatom is common to two different rings. In a bridged heterocyclyl, therings share at least two common non-adjacent atoms. In a fused-ringheterocyclyl, two or more rings may be fused together, such that tworings share one common bond. Examples of fused-ring heterocyclylsinclude hexahydro-furo[3,4-c]pyrrole, hexahydro-furo[3,4-b]pyrrole,octahydro-pyrrolo[3,4-b]pyridine, octahydro-pyrrolo[3,4-c]pyridine,(3aR,6aR)-5-methyl-octahydro-pyrrolo[3,4-b]pyrrole,(3aR,6aR)-octahydro-pyrrolo[3,4-b]pyrrole,6-methyl-2,6-diaza-bicyclo[3.2.0]heptane,(3aS,6aR)-2-methyl-octahydro-pyrrolo[3,4-c]pyrrole,decahydro-[1,5]naphthyridine, 2,3-dihydrobenzofuranyl,2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indolyl, thieno[3,2-c]pyridinyl,furo[3,2-c]pyridinyl, phthalazin-1(2H)-onyl, isoquinolinyl,isoquinolin-1(2H)-onyl, 5,6,7,8-tetrahydrophthalazin-1(2H)-onyl,fluorophthalazin-1(2H)-onyl, (Z)-3H-benzo[d][1,2]diazepin-4(5H)-onyl,(trifluoromethyl)phthalazin-1(2H)-onyl,pyrrolo[1,2-d][1,2,4]triazin-1(2H)-onyl,1,2,3,4-tetrahydroisoquinolinyl, 2,3-dihydrobenzo[b][1,4]dioxinyl,5,6,7,8-tetrahydrophthalazin-1(2H)-onyl,5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazinyl,5,6,7,8-tetrahydroimidazo[1,5-a]pyrazinyl, thieno[3,2-c]pyridinyl,furo[3,2-c]pyridinyl, indolizinyl, pyranopyrrolyl, 4H-quinolizinyl,purinyl, naphthyridinyl, pyridopyridinyl (includingpyrido[3,4-b]-pyridinyl, pyrido[3,2-b]-pyridinyl, orpyrido[4,3-b]-pyridinyl), and pteridinyl. Other examples of fused-ringheterocyclyls include benzo-fused heterocyclyls, such as benzimidazolyl,benzo[d][1,3]dioxolyl, indolyl, isoindolyl (isobenzazolyl,pseudoisoindolyl), indoleninyl (pseudoindolyl), isoindazolyl(benzpyrazolyl), benzazinyl (including quinolinyl (1-benzazinyl) orisoquinolinyl (2-benzazinyl)), phthalazinyl, quinoxalinyl, quinazolinyl,benzodiazinyl (including cinnolinyl (1,2-benzodiazinyl) or quinazolinyl(1,3-benzodiazinyl)), benzopyranyl (including chromanyl orisochromanyl), benzoxazinyl (including 1,3,2-benzoxazinyl,1,4,2-benzoxazinyl, 2,3,1-benzoxazinyl, or 3,1,4-benzoxazinyl), andbenzisoxazinyl (including 1,2-benzisoxazinyl or 1,4-benzisoxazinyl).Examples of spirocyclic heterocyclyls include1,4-dioxa-8-azaspiro[4.5]decanyl.

The term “heterocycloalkyl” (alone or in combination with anotherterm(s)) means a saturated heterocyclyl.

The term “heteroaryl” (alone or in combination with another term(s))means an aromatic heterocyclyl containing from 5 to 14 ring atoms. Aheteroaryl may be a single ring or 2 or 3 fused rings. Examples ofheteroaryl substituents include 6-membered ring substituents such aspyridyl, pyrazyl, pyrimidinyl, pyridazinyl, and 1,3,5-, 1,2,4- or1,2,3-triazinyl; 5-membered ring substituents such as imidazyl, furanyl,thiophenyl, pyrazolyl, oxazolyl, isoxazolyl, thiazolyl, 1,2,3-, 1,2,4-,1,2,5-, or 1,3,4-oxadiazolyl and isothiazolyl; 6/5-membered fused ringsubstituents such as benzothiofuranyl, benzisoxazolyl, benzoxazolyl, andpurinyl; and 6/6-membered fused rings such as benzopyranyl, quinolinyl,isoquinolinyl, cinnolinyl, quinazolinyl, and benzoxazinyl.

A prefix attached to a multi-component substituent only applies to thefirst component. To illustrate, the term “alkylcycloalkyl” contains twocomponents: alkyl and cycloalkyl. Thus, the C₁-C₆— prefix onC₁-C₆-alkylcycloalkyl means that the alkyl component of thealkylcycloalkyl contains from 1 to 6 carbon atoms; the C₁-C₆-prefix doesnot describe the cycloalkyl component. To illustrate further, the prefix“halo” on haloalkyloxyalkyl indicates that only the alkyloxy componentof the alkyloxyalkyl substituent is substituted with one or more halogenradicals. If halogen substitution may alternatively or additionallyoccur on the alkyl component, the substituent would instead be describedas “halogen-substituted alkyloxyalkyl” rather than “haloalkyloxyalkyl.”And finally, if the halogen substitution may only occur on the alkylcomponent, the substituent would instead be described as“alkyloxyhaloalkyl.”

The terms “treat”, “treating” and “treatment” refer to a method ofalleviating or abrogating a disease and/or its attendant symptoms.

The terms “prevent”, “preventing” and “prevention” refer to a method ofpreventing the onset of a disease and/or its attendant symptoms orbarring a subject from acquiring a disease. As used herein, “prevent”,“preventing” and “prevention” also include delaying the onset of adisease and/or its attendant symptoms and reducing a subject's risk ofacquiring a disease.

The term “therapeutically effective amount” refers to that amount of thecompound being administered sufficient to prevent development of oralleviate to some extent one or more of the symptoms of the condition ordisorder being treated.

The term “modulate” refers to the ability of a compound to increase ordecrease the function, or activity, of a kinase. “Modulation”, as usedherein in its various forms, is intended to encompass antagonism,agonism, partial antagonism and/or partial agonism of the activityassociated with kinase. Kinase inhibitors are compounds that, e.g., bindto, partially or totally block stimulation, decrease, prevent, delayactivation, inactivate, desensitize, or down regulate signaltransduction. Kinase activators are compounds that, e.g., bind to,stimulate, increase, open, activate, facilitate, enhance activation,sensitize or up regulate signal transduction.

The term “composition” as used herein is intended to encompass a productcomprising the specified ingredients in the specified amounts, as wellas any product which results, directly or indirectly, from combinationof the specified ingredients in the specified amounts. By“pharmaceutically acceptable” it is meant the carrier, diluent orexcipient must be compatible with the other ingredients of theformulation and not deleterious to the recipient thereof.

The “subject” is defined herein to include animals such as mammals,including, but not limited to, primates (e.g., humans), cows, sheep,goats, horses, dogs, cats, rabbits, rats, mice and the like. Inpreferred embodiments, the subject is a human.

Isotope Enriched or Labeled Compounds

Compounds of the invention can exist in isotope-labeled or -enrichedform containing one or more atoms having an atomic mass or mass numberdifferent from the atomic mass or mass number most abundantly found innature. Isotopes can be radioactive or non-radioactive isotopes.Isotopes of atoms such as hydrogen, carbon, phosphorous, sulfur,fluorine, chlorine, and iodine include, but are not limited to, ²H, ³H,¹³C, ¹⁴C, ¹⁵N, ¹⁸O, ³²P, ³⁵S, ¹⁸F, ³⁶Cl, and ¹²⁵I. Compounds thatcontain other isotopes of these and/or other atoms are within the scopeof this invention.

In another embodiment, the isotope-labeled compounds contain deuterium(²H), tritium (³H) or ¹⁴C isotopes. Isotope-labeled compounds of thisinvention can be prepared by the general methods well known to personshaving ordinary skill in the art. Such isotope-labeled compounds can beconveniently prepared by carrying out the procedures disclosed in theExamples disclosed herein and Schemes by substituting a readilyavailable isotope-labeled reagent for a non-labeled reagent. In someinstances, compounds may be treated with isotope-labeled reagents toexchange a normal atom with its isotope, for example, hydrogen fordeuterium can be exchanged by the action of a deuteric acid such asD₂SO₄/D₂O. In addition to the above, relevant procedures andintermediates are disclosed, for instance, in Lizondo, J et al., DrugsFut, 21(11), 1116 (1996); Brickner, S J et al., J Med Chem, 39(3), 673(1996); Mallesham, B et al., Org Lett, 5(7), 963 (2003); PCTpublications WO1997010223, WO2005099353, WO1995007271, WO2006008754;U.S. Pat. Nos. 7,538,189; 7,534,814; 7,531,685; 7,528,131; 7,521,421;7,514,068; 7,511,013; and US Patent Application Publication Nos.20090137457; 20090131485; 20090131363; 20090118238; 20090111840;20090105338; 20090105307; 20090105147; 20090093422; 20090088416; and20090082471, the methods are hereby incorporated by reference.

The isotope-labeled compounds of the invention may be used as standardsto determine the effectiveness in binding assays. Isotope containingcompounds have been used in pharmaceutical research to investigate thein vivo metabolic fate of the compounds by evaluation of the mechanismof action and metabolic pathway of the nonisotope-labeled parentcompound (Blake et al. J. Pharm. Sci. 64, 3, 367-391 (1975)). Suchmetabolic studies are important in the design of safe, effectivetherapeutic drugs, either because the in vivo active compoundadministered to the patient or because the metabolites produced from theparent compound prove to be toxic or carcinogenic (Foster et al.,Advances in Drug Research Vol. 14, pp. 2-36, Academic press, London,1985; Kato et al., J. Labelled Comp. Radiopharmaceut., 36(10):927-932(1995); Kushner et al., Can. J. Physiol. Pharmacol., 77, 79-88 (1999).

In addition, non-radio active isotope containing drugs, such asdeuterated drugs called “heavy drugs,” can be used for the treatment ofdiseases and conditions related to NAMPT activity. Increasing the amountof an isotope present in a compound above its natural abundance iscalled enrichment. Examples of the amount of enrichment include fromabout 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 16, 21, 25, 29, 33, 37,42, 46, 50, 54, 58, 63, 67, 71, 75, 79, 84, 88, 92, 96, to about 100 mol%. Replacement of up to about 15% of normal atom with a heavy isotopehas been effected and maintained for a period of days to weeks inmammals, including rodents and dogs, with minimal observed adverseeffects (Czajka D M and Finkel A J, Ann. N.Y. Acad. Sci. 1960 84: 770;Thomson J F, Ann. New York Acad. Sci 1960 84: 736; Czakja D M et al.,Am. J. Physiol. 1961 201: 357). Acute replacement of as high as 15%-23%in human fluids with deuterium was found not to cause toxicity(Blagojevic N et al. in “Dosimetry & Treatment Planning for NeutronCapture Therapy”, Zamenhof R, Solares G and Harling O Eds. 1994.Advanced Medical Publishing, Madison Wis. pp. 125-134; Diabetes Metab.23: 251 (1997)).

Stable isotope labeling of a drug can alter its physico-chemicalproperties such as pKa and lipid solubility. These effects andalterations can affect the pharmacodynamic response of the drug moleculeif the isotopic substitution affects a region involved in aligand-receptor interaction. While some of the physical properties of astable isotope-labeled molecule are different from those of theunlabeled one, the chemical and biological properties are the same, withone important exception: because of the increased mass of the heavyisotope, any bond involving the heavy isotope and another atom will bestronger than the same bond between the light isotope and that atom.Accordingly, the incorporation of an isotope at a site of metabolism orenzymatic transformation will slow said reactions potentially alteringthe pharmacokinetic profile or efficacy relative to the non-isotopiccompound.

Compounds

Suitable groups for R¹, R², R³, R⁴, and R⁵ in compounds of Formula (I)are independently selected. The described embodiments of the presentinvention may be combined. Such combination is contemplated and withinthe scope of the present invention. For example, it is contemplated thatembodiments for any of R¹, R², R³, R⁴, and R⁵ can be combined withembodiments defined for any other of R¹, R², R³, R⁴, and R⁵.

Embodiments of Formula (I)

One embodiment of this invention, therefore, pertains to compounds orpharmaceutically acceptable salts thereof, which are useful asinhibitors of NAMPT, the compounds having Formula (I)

wherein

R¹ and R² are each independently selected from the group consisting ofR⁶, C(O)R⁶, C(O)NHR⁶, and C(O)N(R⁶)₂; wherein at least one of R¹ and R²is R⁶; or

R¹ and R², together with the nitrogen to which they are attached form aheterocycloalkyl or heterocycloalkenyl ring; wherein the ring formedwith R¹ and R² together with the nitrogen to which they are attached isoptionally substituted with one or more substituents independentlyselected from the group consisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷,C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷,NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂,NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷,C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂,SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R³, R⁴, and R⁵ are each independently selected from the group consistingof hydrogen, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl,C₁₋₆ hydroxyalkyl, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁶ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR⁸, OR⁸, SR⁸, S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂,NHR⁸, N(R⁸)₂, NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸,NR⁸C(O)OR⁸, NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸,NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸,C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein the aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl represented by R⁶ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁷ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofaryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁷ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁸ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰,OC(O)OR¹⁰, NH₂, NHR¹⁰, N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰,NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰, NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰,NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰, NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰,C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰, C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂,SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂,CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁸ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹, C(O)R¹¹,CO(O)R¹¹, OC(O)R¹¹, OC(O)OR¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹,NR¹¹C(O)R¹¹, NHS(O)₂R¹¹, NR¹¹S(O)₂R¹¹, NHC(O)OR¹¹, NR¹¹C(O)OR¹¹,NHC(O)NH₂, NHC(O)NHR¹¹, NHC(O)N(R¹¹)₂, NR¹¹C(O)NHR¹¹, NR¹¹C(O)N(R¹¹)₂,C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)NHOH, C(O)NHOR¹¹, C(O)NHSO₂R¹¹,C(O)NR¹¹SO₂R¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹¹, C(N)N(R¹¹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁹, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁹ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹², OR¹², SR¹², S(O)R¹², SO₂R¹², C(O)R¹², CO(O)R¹², OC(O)R¹²,OC(O)OR¹², NH₂, NHR¹², N(R¹²)₂, NHC(O)R¹², NR¹²C(O)R¹², NHS(O)₂R¹²,NR¹²S(O)₂R¹², NHC(O)OR¹², NR¹²C(O)OR¹², NHC(O)NH₂, NHC(O)NHR¹²,NHC(O)N(R¹²)₂, NR¹²C(O)NHR¹², NR¹²C(O)N(R¹²)₂, C(O)NH₂, C(O)NHR¹²,C(O)N(R¹²)₂, C(O)NHOH, C(O)NHOR¹², C(O)NHSO₂R¹², C(O)NR¹²SO₂R¹², SO₂NH₂,SO₂NHR¹², SO₂N(R¹²)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR¹², C(N)N(R¹²)₂,CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁹ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³,CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³,NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³,NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂,C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³,C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹³, C(N)N(R¹³)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl,and C₁₋₆ hydroxyalkyl;

R¹¹, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R¹¹ are each independently optionally substituted withone or more substituents independently selected from the groupconsisting of C₁₋₆ alkoxy, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I; wherein the aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl representedby R¹¹ are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of NH₂,C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;

R¹², at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R¹² are each independently optionally substituted withone or more substituents independently selected from the groupconsisting of C₁₋₆ alkoxy, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I; wherein the aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl representedby R¹² are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of NH₂,C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I; and

R¹³, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl; wherein theC₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl represented by R¹³ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of alkoxy, NH₂, C(O)H,C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I.

In one embodiment of Formula (I), R³, R⁴, and R⁵ are each independentlyselected from the group consisting of hydrogen, C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, C₁₋₆ hydroxyalkyl, F, Cl, Br andI. In another embodiment of Formula (I), R³, R⁴, and R⁵ are are eachindependently selected from the group consisting of hydrogen and C₁₋₆alkyl. In another embodiment of Formula (I), one of R³, R⁴, and R⁵ isC₁₋₆ alkyl, and the remainder are hydrogen. In another embodiment ofFormula (I), R³ is C₁₋₆ alkyl, and R⁴ and R⁵ are hydrogen. In anotherembodiment of Formula (I), R⁴ is C₁₋₆ alkyl, and R³ and R⁵ are hydrogen.In another embodiment of Formula (I), R⁵ is C₁₋₆ alkyl, and R³ and R⁴are hydrogen. In another embodiment of Formula (I), R³, R⁴ and R⁵ arehydrogen.

In another embodiment of Formula (I), R³, R⁴, and R⁵ are eachindependently selected from the group consisting of hydrogen and methyl.In another embodiment of Formula (I), one of R³, R⁴, and R⁵ is methyl,and the remainder are hydrogen. In another embodiment of Formula (I), R³is methyl, and R⁴ and R⁵ are hydrogen. In another embodiment of Formula(I), R⁴ is methyl, and R³ and R⁵ are hydrogen. In another embodiment ofFormula (I), R⁵ is methyl, and R³ and R⁴ are hydrogen.

In one embodiment of Formula (I), R¹ and R² are each independentlyselected from the group consisting of R⁶, C(O)R⁶, C(O)NHR⁶, andC(O)N(R⁶)₂; wherein at least one of R¹ and R² is R⁶. In anotherembodiment of Formula (I), R⁶, at each occurrence, is independentlyselected from the group consisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, andC₂₋₆ alkynyl represented by R⁶ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R⁸, OR⁸, SR⁸, S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸,OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂, NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸,NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸, NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂,NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH,C(O)NHOR⁸, C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein the aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl represented by R⁶ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (I), R⁶, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, aryl, heterocycloalkyl, heteroaryl, and cycloalkyl; wherein theC₁₋₆ alkyl, and C₂₋₆ alkenyl represented by R⁶ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R⁸, OR⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸,N(R⁸)₂, NHC(O)R⁸, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)OH, and OH; whereinthe aryl, heterocycloalkyl, heteroaryl, and cycloalkyl represented by R⁶are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of R⁹,OR⁹, C(O)NH₂, C(O)OH, OH, CN, F, Cl, Br and I.

In one embodiment of Formula (I), R⁸, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R⁸ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰,C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰, N(R¹⁰)₂, NHC(O)R¹⁰,NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰, NR¹⁰C(O)OR¹⁰,NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰, NR¹⁰C(O)N(R¹⁰)₂,C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰, C(O)NHSO₂R¹⁰,C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁸ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹,C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, OC(O)OR¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹,NR¹¹C(O)R¹¹, NHS(O)₂R¹¹, NR¹¹S(O)₂R¹¹, NHC(O)OR¹¹, NR¹¹C(O)OR¹¹,NHC(O)NH₂, NHC(O)NHR¹¹, NHC(O)N(R¹¹)₂, NR¹¹C(O)NHR¹¹, NR¹¹C(O)N(R¹¹)₂,C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)NHOH, C(O)NHOR¹¹, C(O)NHSO₂R¹¹,C(O)NR¹¹SO₂R¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹¹, C(N)N(R¹¹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (I), R⁸, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl, andcycloalkyl; wherein the C₁₋₆ alkyl and C₂₋₆ alkenyl represented by R⁸are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of OH, F,Cl, Br and I; wherein the aryl, heterocycloalkyl, and heteroarylrepresented by R⁸ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹¹, OR¹¹, NH₂, N(R¹¹)₂, C(O)H, OH, CN, F, Cl, Br and I.

In one embodiment of Formula (I), R⁹, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R⁹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹², OR¹², SR¹², S(O)R¹², SO₂R¹²,C(O)R¹², CO(O)R¹², OC(O)R¹², OC(O)OR¹², NH₂, NHR¹², N(R¹²)₂, NHC(O)R¹²,NR¹²C(O)R¹², NHS(O)₂R¹², NR¹²S(O)₂R¹², NHC(O)OR¹², NR¹²C(O)OR¹²,NHC(O)NH₂, NHC(O)NHR¹², NHC(O)N(R¹²)₂, NR¹²C(O)NHR¹², NR¹²C(O)N(R¹²)₂,C(O)NH₂, C(O)NHR¹², C(O)N(R¹²)₂, C(O)NHOH, C(O)NHOR¹², C(O)NHSO₂R¹²,C(O)NR¹²SO₂R¹², SO₂NH₂, SO₂NHR¹², SO₂N(R¹²)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹², C(N)N(R¹²)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³,C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³,NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³,NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂,C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³,C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹³, C(N)N(R¹³)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (I), R⁹, at each occurrence, is C₁₋₆alkyl.

In one embodiment of Formula (I), R¹⁰, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, and C₁₋₆ hydroxyalkyl.

In one embodiment of Formula (I), R¹¹, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R¹¹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of C₁₋₆ alkoxy, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R¹¹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I. In another embodiment of Formula (I), R¹¹, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl, C₂₋₆ alkenyl, aryl, and heteroaryl; wherein the C₁₋₆ alkyl andC₂₋₆ alkenyl represented by R¹¹ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of C₁₋₆ alkoxy, cycloalkyl, OH, F, Cl, Br and I.

In one embodiment of Formula (I), R¹², at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R¹² are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of C₁₋₆ alkoxy, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R¹² are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I.

In one embodiment of Formula (I), R¹³, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, andC₂₋₆ alkynyl represented by R¹³ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of alkoxy, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F,Cl, Br and I.

In another embodiment of Formula (I), R¹ is C(O)R⁶; and R² is R⁶. Inanother embodiment of Formula (I), R⁶, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, aryl,heterocycloalkyl, heteroaryl, and cycloalkyl; wherein the C₁₋₆ alkylrepresented by R⁶ is independently optionally substituted with one ormore substituents independently selected from the group consisting ofR⁸, OR⁸, C(O)R⁸, OC(O)R⁸, N(R⁸)₂, NHC(O)R⁸, C(O)NHR⁸, and OH; whereinthe aryl, heterocycloalkyl, and heteroaryl represented by R⁶ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁹, OR⁹, C(O)NH₂,OH, CN, F, Cl, Br and I. In another embodiment of Formula (I), R⁸, ateach occurrence, is independently selected from the group consisting ofC₁₋₆ alkyl, C₂₋₆ alkenyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, and cycloalkyl; wherein the aryl, heterocycloalkyl, andheteroaryl represented by R⁸ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹¹, OR¹¹, NH₂, N(R¹¹)₂, C(O)H, OH, CN, F, Cl,Br and I. In another embodiment of Formula (I), R⁹, at each occurrence,is C₁₋₆ alkyl. In another embodiment of Formula (I), R¹¹, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl, C₂₋₆ alkenyl, and aryl; wherein the C₁₋₆ alkyl and C₂₋₆ alkenylrepresented by R¹¹ are each independently optionally substituted withone or more substituents independently selected from the groupconsisting of C₁₋₆ alkoxy, cycloalkyl, OH, F, Cl, Br and I.

In another embodiment of Formula (I), R¹ and R² are each R⁶. In anotherembodiment of Formula (I), R⁶, at each occurrence, is C₁₋₆ alkyl;wherein the C₁₋₆ alkyl represented by R⁶ is independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R⁸, C(O)R⁸, C(O)NHR⁸, and C(O)N(R⁸)₂. In anotherembodiment of Formula (I), R⁸, at each occurrence, is independentlyselected from the group consisting of C₁₋₆ alkyl, aryl, andheterocycloalkyl; wherein the aryl, and heterocycloalkyl represented byR⁸ are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of R¹¹,CN, F, Cl, Br and I. In another embodiment of Formula (I), R¹¹, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl and heteroaryl.

In another embodiment of Formula (I), R¹ is C(O)NHR⁶; and R² is R⁶. Inanother embodiment of Formula (I), R⁶, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, heterocycloalkyl, and cycloalkyl; wherein the C₁₋₆ alkyl andC₂₋₆ alkenyl represented by R⁶ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R⁸, OR⁸, C(O)OR⁸, N(R⁸)₂, NHC(O)R⁸, C(O)NH₂,C(O)N(R⁸)₂, C(O)OH, and OH; wherein the heterocycloalkyl, and cycloalkylrepresented by R⁶ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofC(O)NH₂, C(O)OH, F, Cl, Br and I. In another embodiment of Formula (I),R⁸, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, aryl, heterocycloalkyl, and heteroaryl;wherein the C₁₋₆ alkyl represented by R⁸ is independently optionallysubstituted with one or more OH; wherein the aryl, heterocycloalkyl, andheteroaryl represented by R⁸ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of OH, CN, F, Cl, Br and I.

In another embodiment of Formula (I), R¹ is C(O)N(R⁶)₂; and R² is R⁶. Inanother embodiment of Formula (I), R⁶, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, heterocycloalkyl, and cycloalkyl; wherein the C₁₋₆ alkyl andC₂₋₆ alkenyl represented by R⁶ are independently optionally substitutedwith one or more substituents independently selected from the groupconsisting of R⁸, OR⁸, C(O)OR⁸, N(R⁸)₂, NHC(O)R⁸, C(O)NH₂, C(O)N(R⁸)₂,C(O)OH, and OH; wherein the heterocycloalkyl, and cycloalkyl representedby R⁶ are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of OH, F,Cl, Br and I. In another embodiment of Formula (I), R⁸, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl, aryl, and heterocycloalkyl; wherein the C₁₋₆ alkyl represented byR⁸ is independently optionally substituted with one or more OH; whereinthe aryl and heterocycloalkyl represented by R⁸ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of OH, CN, F, Cl, Br and I.

In another embodiment of Formula (I), R⁶, at each occurrence, is C₁₋₆alkyl; wherein the C₁₋₆ alkyl represented by R⁶ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R⁸, and OR⁸. In another embodimentof Formula (I), R⁸, at each occurrence, is independently selected fromthe group consisting of C₁₋₆ alkyl, and aryl; wherein the arylrepresented by R⁸ is independently optionally substituted with one ormore substituents independently selected from the group consisting of F,Cl, Br and I.

In another embodiment of Formula (I), R¹ and R², together with thenitrogen to which they are attached form a heterocycloalkyl orheterocycloalkenyl ring. In another embodiment of Formula (I), R¹ andR², together with the nitrogen to which they are attached form aheterocycloalkyl ring. In another embodiment of Formula (I), R⁷, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl; whereinthe C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl represented by R⁷ areeach independently optionally substituted with one or more substituentsindependently selected from the group consisting of aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁷ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I. In another embodiment of Formula (I), R¹ and R²,together with the nitrogen to which they are attached form aheterocycloalkyl ring wherein the ring formed with R¹ and R² togetherwith the nitrogen to which they are attached is optionally substitutedwith one or more R⁷. In another embodiment of Formula (I), R⁷, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl; whereinthe C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl represented by R⁷ areeach independently optionally substituted with one or more substituentsindependently selected from the group consisting of aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁷ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I. In another embodiment of Formula (I), R⁷, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl, and aryl; wherein the C₁₋₆ alkyl represented by R⁷ isindependently optionally substituted with one or more substituentsindependently selected from the group consisting of aryl and OH; whereinthe aryl represented by R⁷ is independently optionally substituted withone or more substituents independently selected from the groupconsisting of F, Cl, Br and I.

Still another embodiment pertains to compounds having Formula (I), whichinclude

-   2-{(4-fluorobenzyl)[4-(pyridin-3-yl)benzyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{methyl[4-(pyridin-3-yl)benzyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(methyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(tetrahydro-2H-pyran-4-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(cyclohexylacetyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(3-methylbutanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[3-(morpholin-4-yl)propyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[3-(piperidin-1-yl)propyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[2-(pyrrolidin-1-yl)ethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){2-[4-(propan-2-yl)piperazin-1-yl]ethyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzoyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(3-chlorobenzoyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzoyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(5-chloro-1,3-benzodioxol-4-yl)methyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-chlorobenzyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(2-chlorobenzyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(2,5-dichlorobenzyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[2-(methylamino)-2-oxoethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[2-oxo-2-(propan-2-ylamino)ethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(dimethylamino)-2-oxoethyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(diethylamino)-2-oxoethyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[2-(morpholin-4-yl)-2-oxoethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(4-methylbenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(methoxyacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(N,N-dimethylglycyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(3,6-dihydropyridin-1(2H)-ylacetyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(4-methylpiperidin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(4-hydroxypiperidin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(4-methylpiperazin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[4-(propan-2-yl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(4-formylpiperazin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(hexahydropyrrolo[1,2-a]pyrazin-2(1H)-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[4-(cyclopropylmethyl)piperazin-1-yl]acetyl}(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[4-(2-ethoxyethyl)piperazin-1-yl]acetyl}(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(cyclopropylcarbonyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[4-(prop-2-en-1-yl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[4-(3-methoxypropyl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[3-(dimethylamino)pyrrolidin-1-yl]acetyl}(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(morpholin-4-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(3-hydroxypiperidin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[4-(2-hydroxyethyl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(1,4-dioxa-7-azaspiro[4.4]non-7-ylacetyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   1-{2-[(4-fluorobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)amino]-2-oxoethyl}pyridinium;-   2-{[2-(4-fluorophenyl)ethyl](3-methylbutanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(propan-2-ylcarbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(4-cyanophenyl)ethyl](3-methylbutanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(4-cyanophenyl)ethyl](tetrahydro-2H-pyran-4-ylacetyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methylbutanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(tetrahydro-2H-pyran-4-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(4-cyanophenyl)ethyl](tetrahydrofuran-3-ylacetyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(3-methylbutanoyl)amino]-N-[3-(2-methyl-1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(3-methylbutanoyl)amino]-N-[3-(4-methyl-1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(2-fluorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(3-fluorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(2-chlorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(3-chlorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-chlorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(tetrahydrofuran-3-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(3-methylbutyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-methylpropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N¹-(4-fluorobenzyl)-N¹-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)piperidine-1,3-dicarboxamide;-   2-{(4-fluorobenzyl)[(3-hydroxyazetidin-1-yl)carbonyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-1,4-dioxa-7-azaspiro[4.4]nonane-7-carboxamide;-   2-{(4-fluorobenzyl)[(3-methoxypyrrolidin-1-yl)carbonyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-methoxyethyl)(methyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-2,6-dimethylmorpholine-4-carboxamide;-   2-{[ethyl(2-methoxyethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-2,2-dimethylmorpholine-4-carboxamide;-   N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-1,4-oxazepane-4-carboxamide;-   2-[(4-fluorobenzoyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(4-methylbenzyl)amino]-1,3-thiazole-5-carboxamide;-   N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-N-(3-methylbutyl)-1,2-oxazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(2-phenoxypropanoyl)amino]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-propoxyethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(tetrahydrofuran-2-ylmethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(1-methoxypropan-2-yl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-methoxyethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(2-ethoxyethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(1-methoxybutan-2-yl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(4-cyanophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(1,3-dioxolan-2-ylmethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[2-(propan-2-yloxy)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(1,4-dioxan-2-ylmethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(1,3-dimethoxypropan-2-yl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-methoxybutyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(tetrahydrofuran-3-ylcarbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(tetrahydro-2H-pyran-3-ylcarbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(pyrimidin-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(2-methoxypyridin-4-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(1,3-oxazol-4-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   2-{[(5-chloropyridin-2-yl)methyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(4-methylpyridin-3-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(6-methoxypyridin-3-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(4-methyl-1,3-thiazol-5-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[2-(3-hydroxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(pyridin-2-yl)ethyl]amino}-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(1,3-benzodioxol-5-yl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(4-chlorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(3-fluorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(4-hydroxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(3-chlorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   N-[3-(1H-imidazol-1-yl)propyl]-2-{[2-(3-methoxyphenyl)ethyl](3-methoxypropanoyl)amino}-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(2-fluorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-hydroxy-2-(4-methoxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[1-(pyridin-2-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(1-methyl-1H-pyrazol-4-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(2,6-difluorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(6-methylpyridin-3-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(4-chlorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(5-methylpyrazin-2-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(3-chlorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(5-methylpyridin-2-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(2,5-difluorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(2-methylbenzyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(3-methylbenzyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(pyridin-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(pyridin-3-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[2-(propan-2-yloxy)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(2-methoxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[2-(2-hydroxyethoxy)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(propan-2-yloxy)propyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(3-hydroxy-2,2-dimethylpropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(2-hydroxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(1-hydroxypropan-2-yl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(3-hydroxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[(2S)-1-hydroxybut-3-en-2-yl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(4-hydroxybutyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methylbutyl)[(2R)-2-phenoxypropanoyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methylbutyl)[(2S)-2-phenoxypropanoyl]amino}-1,3-thiazole-5-carboxamide;-   N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-5-methyl-N-(3-methylbutyl)-1,2-oxazole-3-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(phenoxyacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(3-phenylpropanoyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(2-phenylpropanoyl)amino]-1,3-thiazole-5-carboxamide;-   2-{[(4-fluorophenyl)acetyl](3-methylbutyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(3-amino-3-oxopropyl)carbamoyl](4-cyanobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[3-(acetylamino)-2-methylpropyl]carbamoyl}(4-cyanobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(dimethylamino)-3-oxopropyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(3-ethoxy-2-hydroxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(diethylamino)propyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[2-(acetylamino)ethyl]carbamoyl}(4-cyanobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[2-(diethylamino)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)({2-[(2-methylpropanoyl)amino]ethyl}carbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[(2R)-1-hydroxybut-3-en-2-yl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(3-hydroxyazetidin-1-yl)propyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(3-methylbutyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(methoxyacetyl)(3-methylbutyl)amino]-1,3-thiazole-5-carboxamide;-   2-[(cyclopropylcarbonyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   (2S)-1-[(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)(3-methylbutyl)amino]-1-oxopropan-2-yl    acetate;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydro-2H-pyran-4-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydrofuran-3-ylcarbonyl)amino]-1,3-thiazole-5-carboxamide;-   2-{[2-hydroxy-2-(3-methoxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(pyrazin-2-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[1-(3-hydroxyphenyl)propan-2-yl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   ethyl    N-[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]-beta-alaninate;-   ethyl    4-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoate;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoate;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-4-methylpentanoate;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2,2-dimethylpropanoate;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}cyclobutanecarboxylic    acid;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2-methylpropanoate;-   2-{(4-cyanobenzyl)[(3-methoxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoic    acid;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-4-methylpentanoic    acid;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2,2-dimethylpropanoic    acid;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2-methylpropanoic    acid;-   N-[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]-beta-alanine;-   4-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoic    acid;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydrofuran-2-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydrofuran-3-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(3-methoxypropanoyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(3-methoxypropyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(tetrahydro-2H-pyran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(tetrahydrofuran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(propan-2-yloxy)ethyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[2-(1,3-dioxolan-2-yl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(1,4-dioxan-2-ylmethyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[3-(4-fluorophenyl)propanoyl](2-methoxyethyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(2-methoxyethyl)[3-(pyridin-3-yl)propanoyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(pyridin-3-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(naphthalen-2-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(2-methoxyethyl)[(4-phenoxyphenyl)acetyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[(4-cyanophenyl)acetyl](2-methoxyethyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(4-aminophenyl)acetyl](2-methoxyethyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{2-[di(prop-2-en-1-yl)amino]ethyl}(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[3-(diethylamino)propyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(diethylamino)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-(pyrrolidin-1-yl)propyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[(1-ethyl-5-oxopyrrolidin-3-yl)methyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(5-oxopyrrolidin-2-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-oxo-3-(pyrrolidin-1-yl)propyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-oxo-2-(piperidin-1-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-(2-oxopyrrolidin-1-yl)propyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(2-oxo-1,3-oxazolidin-3-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl){2-[(2-methylpropanoyl)amino]ethyl}amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-(methylamino)-3-oxopropyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[3-(acetylamino)propyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-oxo-2-(pyrrolidin-1-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   2-[3-(2-hydroxyethyl)-2-oxoimidazolidin-1-yl]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[3-(4-fluorophenyl)-2-oxoimidazolidin-1-yl]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(5-chloropyridin-2-yl)methyl](tetrahydro-2H-pyran-4-ylcarbonyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(5-chloropyridin-2-yl)methyl](tetrahydrofuran-3-ylcarbonyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(5-chloropyridin-2-yl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(5-chloropyridin-2-yl)ethyl](tetrahydrofuran-3-ylcarbonyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(5-chloropyridin-2-yl)ethyl][(2-methoxy    ethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-([2-(5-chloropyridin-2-yl)ethyl]{[2-(propan-2-yloxy)ethyl]carbamoyl}amino)-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(1,3-benzodioxol-5-ylacetyl)(2-methoxyethyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(5S)-5-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-2-oxo-1,3-oxazolidin-3-yl}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(pyridin-2-ylacetyl)amino]-1,3-thiazole-5-carboxamide;    and pharmaceutically acceptable salts thereof.

Embodiments of Formula (II)

In another aspect, the present invention provides compounds of Formula(II)

and pharmaceutically acceptable salts thereof; wherein R¹ and R² are asdescribed herein for Formula (I).

One embodiment of this invention pertains to compounds of Formula (II)or pharmaceutically acceptable salts thereof;

wherein

R¹ and R² are each independently selected from the group consisting ofR⁶, C(O)R⁶, C(O)NHR⁶, and C(O)N(R⁶)₂; wherein at least one of R¹ and R²is R⁶; or

R¹ and R², together with the nitrogen to which they are attached form aheterocycloalkyl or heterocycloalkenyl ring; wherein the ring formedwith R¹ and R² together with the nitrogen to which they are attached isoptionally substituted with one or more substituents independentlyselected from the group consisting of R⁷, OR⁷, SR⁷, S(O)R⁷, SO₂R⁷,C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷, N(R⁷)₂, NHC(O)R⁷,NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷, NR⁷C(O)OR⁷, NHC(O)NH₂,NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷, NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷,C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷, C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂,SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁶, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁶ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR⁸, OR⁸, SR⁸, S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂,NHR⁸, N(R⁸)₂, NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸,NR⁸C(O)OR⁸, NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸,NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸,C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein the aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl represented by R⁶ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁷, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁷ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofaryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁷ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁸ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰,OC(O)OR¹⁰, NH₂, NHR¹⁰, N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰,NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰, NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰,NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰, NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰,C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰, C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂,SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂,CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁸ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹, C(O)R¹¹,CO(O)R¹¹, OC(O)R¹¹, OC(O)OR¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹,NR¹¹C(O)R¹¹, NHS(O)₂R¹¹, NR¹¹S(O)₂R¹¹, NHC(O)OR¹¹, NR¹¹C(O)OR¹¹,NHC(O)NH₂, NHC(O)NHR¹¹, NHC(O)N(R¹¹)₂, NR¹¹C(O)NHR¹¹, NR¹¹C(O)N(R¹¹)₂,C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)NHOH, C(O)NHOR¹¹, C(O)NHSO₂R¹¹,C(O)NR¹¹SO₂R¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹¹, C(N)N(R¹¹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁹, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁹ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹², OR¹², SR¹², S(O)R¹², SO₂R¹², C(O)R¹², CO(O)R¹², OC(O)R¹²,OC(O)OR¹², NH₂, NHR¹², N(R¹²)₂, NHC(O)R¹², NR¹²C(O)R¹², NHS(O)₂R¹²,NR¹²S(O)₂R¹², NHC(O)OR¹², NR¹²C(O)OR¹², NHC(O)NH₂, NHC(O)NHR¹²,NHC(O)N(R¹²)₂, NR¹²C(O)NHR¹², NR¹²C(O)N(R¹²)₂, C(O)NH₂, C(O)NHR¹²,C(O)N(R¹²)₂, C(O)NHOH, C(O)NHOR¹², C(O)NHSO₂R¹², C(O)NR¹²SO₂R¹², SO₂NH₂,SO₂NHR¹², SO₂N(R¹²)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR¹², C(N)N(R¹²)₂,CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁹ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³,CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³,NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³,NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂,C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³,C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹³, C(N)N(R¹³)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl,and C₁₋₆ hydroxyalkyl;

R¹¹, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R¹¹ are each independently optionally substituted withone or more substituents independently selected from the groupconsisting of C₁₋₆ alkoxy, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I; wherein the aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl representedby R¹¹ are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of NH₂,C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;

R¹², at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R¹² are each independently optionally substituted withone or more substituents independently selected from the groupconsisting of C₁₋₆ alkoxy, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I; wherein the aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl representedby R¹² are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of NH₂,C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I; and

R¹³, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl; wherein theC₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl represented by R¹³ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of alkoxy, NH₂, C(O)H,C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I.

In one embodiment of Formula (II), R¹ and R² are each independentlyselected from the group consisting of R⁶, C(O)R⁶, C(O)NHR⁶, andC(O)N(R⁶)₂; wherein at least one of R¹ and R² is R⁶. In anotherembodiment of Formula (II), R⁶, at each occurrence, is independentlyselected from the group consisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, andC₂₋₆ alkynyl represented by R⁶ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R⁸, OR⁸, SR⁸, S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸,OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂, NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸,NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸, NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂,NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH,C(O)NHOR⁸, C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; wherein the aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl represented by R⁶ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (II), R⁶, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, aryl, heterocycloalkyl, heteroaryl, and cycloalkyl; wherein theC₁₋₆ alkyl, and C₂₋₆ alkenyl represented by R⁶ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R⁸, OR⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸,N(R⁸)₂, NHC(O)R⁸, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)OH, and OH; whereinthe aryl, heterocycloalkyl, heteroaryl, and cycloalkyl represented by R⁶are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of R⁹,OR⁹, C(O)NH₂, C(O)OH, OH, CN, F, Cl, Br and I.

In one embodiment of Formula (II), R⁸, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R⁸ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰,C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰, N(R¹⁰)₂, NHC(O)R¹⁰,NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰, NR¹⁰C(O)OR¹⁰,NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰, NR¹⁰C(O)N(R¹⁰)₂,C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰, C(O)NHSO₂R¹⁰,C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁸ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹,C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, OC(O)OR¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹,NR¹¹C(O)R¹¹, NHS(O)₂R¹¹, NR¹¹S(O)₂R¹¹, NHC(O)OR¹¹, NR¹¹C(O)OR¹¹,NHC(O)NH₂, NHC(O)NHR¹¹, NHC(O)N(R¹¹)₂, NR¹¹C(O)NHR¹¹, NR¹¹C(O)N(R¹¹)₂,C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)NHOH, C(O)NHOR¹¹, C(O)NHSO₂R¹¹,C(O)NR¹¹SO₂R¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹¹, C(N)N(R¹¹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (II), R⁸, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl, andcycloalkyl; wherein the C₁₋₆ alkyl and C₂₋₆ alkenyl represented by R⁸are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of OH, F,Cl, Br and I; wherein the aryl, heterocycloalkyl, and heteroarylrepresented by R⁸ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹¹, OR¹¹, NH₂, N(R¹¹)₂, C(O)H, OH, CN, F, Cl, Br and I.

In one embodiment of Formula (II), R⁹, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R⁹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹², OR¹², SR¹², S(O)R¹², SO₂R¹²,C(O)R¹², CO(O)R¹², OC(O)R¹², OC(O)OR¹², NH₂, NHR¹², N(R¹²)₂, NHC(O)R¹²,NR¹²C(O)R¹², NHS(O)₂R¹², NR¹²S(O)₂R¹², NHC(O)OR¹², NR¹²C(O)OR¹²,NHC(O)NH₂, NHC(O)NHR¹², NHC(O)N(R¹²)₂, NR¹²C(O)NHR¹², NR¹²C(O)N(R¹²)₂,C(O)NH₂, C(O)NHR¹², C(O)N(R¹²)₂, C(O)NHOH, C(O)NHOR¹², C(O)NHSO₂R¹²,C(O)NR¹²SO₂R¹², SO₂NH₂, SO₂NHR¹², SO₂N(R¹²)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹², C(N)N(R¹²)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³,C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³,NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³,NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂,C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³,C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹³, C(N)N(R¹³)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (II), R⁹, at each occurrence, is C₁₋₆alkyl.

In one embodiment of Formula (II), R¹⁰, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, and C₁₋₆ hydroxyalkyl.

In one embodiment of Formula (II), R¹¹, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R¹¹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of C₁₋₆ alkoxy, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R¹¹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I. In another embodiment of Formula (II), R¹¹, ateach occurrence, is independently selected from the group consisting ofC₁₋₆ alkyl, C₂₋₆ alkenyl, aryl, and heteroaryl; wherein the C₁₋₆ alkyland C₂₋₆ alkenyl represented by R¹¹ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of C₁₋₆ alkoxy, cycloalkyl, OH, F, Cl, Br and I.

In one embodiment of Formula (II), R¹², at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R¹² are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of C₁₋₆ alkoxy, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R¹² are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I.

In one embodiment of Formula (II), R¹³, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, andC₂₋₆ alkynyl represented by R¹³ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of alkoxy, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F,Cl, Br and I.

In another embodiment of Formula (II), R¹ is C(O)R⁶; and R² is R⁶. Inanother embodiment of Formula (II), R⁶, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, aryl,heterocycloalkyl, heteroaryl, and cycloalkyl; wherein the C₁₋₆ alkylrepresented by R⁶ is independently optionally substituted with one ormore substituents independently selected from the group consisting ofR⁸, OR⁸, C(O)R⁸, OC(O)R⁸, N(R⁸)₂, NHC(O)R⁸, C(O)NHR⁸, and OH; whereinthe aryl, heterocycloalkyl, and heteroaryl represented by R⁶ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁹, OR⁹, C(O)NH₂,OH, CN, F, Cl, Br and I. In another embodiment of Formula (II), R⁸, ateach occurrence, is independently selected from the group consisting ofC₁₋₆ alkyl, C₂₋₆ alkenyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, and cycloalkyl; wherein the aryl, heterocycloalkyl, andheteroaryl represented by R⁸ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹¹, OR¹¹, NH₂, N(R¹¹)₂, C(O)H, OH, CN, F, Cl,Br and I. In another embodiment of Formula (II), R⁹, at each occurrence,is C₁₋₆ alkyl. In another embodiment of Formula (II), R¹¹, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl, C₂₋₆ alkenyl, and aryl; wherein the C₁₋₆ alkyl and C₂₋₆ alkenylrepresented by R¹¹ are each independently optionally substituted withone or more substituents independently selected from the groupconsisting of C₁₋₆ alkoxy, cycloalkyl, OH, F, Cl, Br and I.

In another embodiment of Formula (II), R¹ and R² are each R⁶. In anotherembodiment of Formula (II), R⁶, at each occurrence, is C₁₋₆ alkyl;wherein the C₁₋₆ alkyl represented by R⁶ is independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R⁸, C(O)R⁸, C(O)NHR⁸, and C(O)N(R⁸)₂. In anotherembodiment of Formula (II), R⁸, at each occurrence, is independentlyselected from the group consisting of C₁₋₆ alkyl, aryl, andheterocycloalkyl; wherein the aryl, and heterocycloalkyl represented byR⁸ are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of R¹¹,CN, F, Cl, Br and I. In another embodiment of Formula (II), R¹¹, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl and heteroaryl.

In another embodiment of Formula (II), R¹ is C(O)NHR⁶; and R² is R⁶. Inanother embodiment of Formula (II), R⁶, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, heterocycloalkyl, and cycloalkyl; wherein the C₁₋₆ alkyl andC₂₋₆ alkenyl represented by R⁶ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R⁸, OR⁸, C(O)OR⁸, N(R⁸)₂, NHC(O)R⁸, C(O)NH₂,C(O)N(R⁸)₂, C(O)OH, and OH; wherein the heterocycloalkyl, and cycloalkylrepresented by R⁶ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofC(O)NH₂, C(O)OH, F, Cl, Br and I. In another embodiment of Formula (II),R⁸, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, aryl, heterocycloalkyl, and heteroaryl;wherein the C₁₋₆ alkyl is independently optionally substituted with oneor more OH; wherein the aryl, heterocycloalkyl, and heteroarylrepresented by R⁸ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofOH, CN, F, Cl, Br and I.

In another embodiment of Formula (II), R¹ is C(O)N(R⁶)₂; and R² is R⁶.In another embodiment of Formula (II), R⁶, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, heterocycloalkyl, and cycloalkyl; wherein the C₁₋₆ alkyl andC₂₋₆ alkenyl represented by R⁶ are independently optionally substitutedwith one or more substituents independently selected from the groupconsisting of R⁸, OR⁸, C(O)OR⁸, N(R⁸)₂, NHC(O)R⁸, C(O)NH₂, C(O)N(R⁸)₂,C(O)OH, and OH; wherein the heterocycloalkyl, and cycloalkyl representedby R⁶ are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of OH, F,Cl, Br and I. In another embodiment of Formula (II), R⁸, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl, aryl, and heterocycloalkyl; wherein the C₁₋₆ alkyl isindependently optionally substituted with one or more OH; wherein thearyl and heterocycloalkyl represented by R⁸ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of OH, CN, F, Cl, Br and I.

In another embodiment of Formula (II), R¹ and R², together with thenitrogen to which they are attached form a heterocycloalkyl orheterocycloalkenyl ring. In another embodiment of Formula (II), R¹ andR², together with the nitrogen to which they are attached form aheterocycloalkyl ring. In another embodiment of Formula (II), R⁷, ateach occurrence, is independently selected from the group consisting ofC₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl; whereinthe C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl represented by R⁷ areeach independently optionally substituted with one or more substituentsindependently selected from the group consisting of aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁷ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I. In another embodiment of Formula (II), R¹ and R²,together with the nitrogen to which they are attached form aheterocycloalkyl ring wherein the ring formed with R¹ and R² togetherwith the nitrogen to which they are attached is optionally substitutedwith one or more R⁷. In another embodiment of Formula (II), R⁷, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl; whereinthe C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl represented by R⁷ areeach independently optionally substituted with one or more substituentsindependently selected from the group consisting of aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁷ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I. In another embodiment of Formula (II), R⁷, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl, and aryl; wherein the C₁₋₆ alkyl is independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of aryl and OH; wherein the aryl represented by R⁷is independently optionally substituted with one or more substituentsindependently selected from the group consisting of F, Cl, Br and I.

Still another embodiment pertains to compounds having Formula (II),which include

-   2-{(4-fluorobenzyl)[4-(pyridin-3-yl)benzyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{methyl[4-(pyridin-3-yl)benzyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(methyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(tetrahydro-2H-pyran-4-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(cyclohexylacetyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(3-methylbutanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[3-(morpholin-4-yl)propyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[3-(piperidin-1-yl)propyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[2-(pyrrolidin-1-yl)ethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){2-[4-(propan-2-yl)piperazin-1-yl]ethyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzoyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(3-chlorobenzoyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzoyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(5-chloro-1,3-benzodioxol-4-yl)methyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-chlorobenzyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(2-chlorobenzyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(2,5-dichlorobenzyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[2-(methylamino)-2-oxoethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[2-oxo-2-(propan-2-ylamino)ethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(dimethylamino)-2-oxoethyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(diethylamino)-2-oxoethyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[2-(morpholin-4-yl)-2-oxoethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(4-methylbenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(methoxyacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(N,N-dimethylglycyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(3,6-dihydropyridin-1(2H)-ylacetyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(4-methylpiperidin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(4-hydroxypiperidin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(4-methylpiperazin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[4-(propan-2-yl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(4-formylpiperazin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(hexahydropyrrolo[1,2-a]pyrazin-2(1H)-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[4-(cyclopropylmethyl)piperazin-1-yl]acetyl}(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[4-(2-ethoxyethyl)piperazin-1-yl]acetyl}(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(cyclopropylcarbonyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[4-(prop-2-en-1-yl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[4-(3-methoxypropyl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[3-(dimethylamino)pyrrolidin-1-yl]acetyl}(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(morpholin-4-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(3-hydroxypiperidin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[4-(2-hydroxyethyl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(1,4-dioxa-7-azaspiro[4.4]non-7-ylacetyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   1-{2-[(4-fluorobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)amino]-2-oxoethyl}pyridinium;-   2-{[2-(4-fluorophenyl)ethyl](3-methylbutanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(propan-2-ylcarbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(4-cyanophenyl)ethyl](3-methylbutanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(4-cyanophenyl)ethyl](tetrahydro-2H-pyran-4-ylacetyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methylbutanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(tetrahydro-2H-pyran-4-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(4-cyanophenyl)ethyl](tetrahydrofuran-3-ylacetyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(2-fluorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(3-fluorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(2-chlorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(3-chlorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-chlorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(tetrahydrofuran-3-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(3-methylbutyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-methylpropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;

N¹-(4-fluorobenzyl)-N¹-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)piperidine-1,3-dicarboxamide;

-   2-{(4-fluorobenzyl)[(3-hydroxyazetidin-1-yl)carbonyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-1,4-dioxa-7-azaspiro[4.4]nonane-7-carboxamide;-   2-{(4-fluorobenzyl)[(3-methoxypyrrolidin-1-yl)carbonyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-methoxyethyl)(methyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-2,6-dimethylmorpholine-4-carboxamide;-   2-{[ethyl(2-methoxyethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-2,2-dimethylmorpholine-4-carboxamide;-   N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-1,4-oxazepane-4-carboxamide;-   2-[(4-fluorobenzoyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(4-methylbenzyl)amino]-1,3-thiazole-5-carboxamide;-   N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-N-(3-methylbutyl)-1,2-oxazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(2-phenoxypropanoyl)amino]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-propoxyethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(tetrahydrofuran-2-ylmethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(1-methoxypropan-2-yl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-methoxyethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(2-ethoxyethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(1-methoxybutan-2-yl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(4-cyanophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(1,3-dioxolan-2-ylmethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[2-(propan-2-yloxy)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(1,4-dioxan-2-ylmethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(1,3-dimethoxypropan-2-yl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-methoxybutyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(tetrahydrofuran-3-ylcarbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(tetrahydro-2H-pyran-3-ylcarbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(pyrimidin-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(2-methoxypyridin-4-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(1,3-oxazol-4-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   2-{[(5-chloropyridin-2-yl)methyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(4-methylpyridin-3-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(6-methoxypyridin-3-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(4-methyl-1,3-thiazol-5-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[2-(3-hydroxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(pyridin-2-yl)ethyl]amino}-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(1,3-benzodioxol-5-yl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(4-chlorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(3-fluorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(4-hydroxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(3-chlorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   N-[3-(1H-imidazol-1-yl)propyl]-2-{[2-(3-methoxyphenyl)ethyl](3-methoxypropanoyl)amino}-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(2-fluorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-hydroxy-2-(4-methoxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[1-(pyridin-2-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(1-methyl-1H-pyrazol-4-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(2,6-difluorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(6-methylpyridin-3-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(4-chlorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(5-methylpyrazin-2-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(3-chlorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(5-methylpyridin-2-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(2,5-difluorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(2-methylbenzyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(3-methylbenzyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(pyridin-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(pyridin-3-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[2-(propan-2-yloxy)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(2-methoxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[2-(2-hydroxyethoxy)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(propan-2-yloxy)propyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(3-hydroxy-2,2-dimethylpropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(2-hydroxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(1-hydroxypropan-2-yl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(3-hydroxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[(2S)-1-hydroxybut-3-en-2-yl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(4-hydroxybutyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methylbutyl)[(2R)-2-phenoxypropanoyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methylbutyl)[(2S)-2-phenoxypropanoyl]amino}-1,3-thiazole-5-carboxamide;-   N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-5-methyl-N-(3-methylbutyl)-1,2-oxazole-3-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(phenoxyacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(3-phenylpropanoyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(2-phenylpropanoyl)amino]-1,3-thiazole-5-carboxamide;-   2-{[(4-fluorophenyl)acetyl](3-methylbutyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(3-amino-3-oxopropyl)carbamoyl](4-cyanobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[3-(acetylamino)-2-methylpropyl]carbamoyl}(4-cyanobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(dimethylamino)-3-oxopropyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(3-ethoxy-2-hydroxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(diethylamino)propyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[2-(acetylamino)ethyl]carbamoyl}(4-cyanobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[2-(diethylamino)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)({2-[(2-methylpropanoyl)amino]ethyl}carbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[(2R)-1-hydroxybut-3-en-2-yl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(3-hydroxyazetidin-1-yl)propyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(3-methylbutyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(methoxyacetyl)(3-methylbutyl)amino]-1,3-thiazole-5-carboxamide;-   2-[(cyclopropylcarbonyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   (2S)-1-[(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)(3-methylbutyl)amino]-1-oxopropan-2-yl    acetate;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydro-2H-pyran-4-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydrofuran-3-ylcarbonyl)amino]-1,3-thiazole-5-carboxamide;-   2-{[2-hydroxy-2-(3-methoxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(pyrazin-2-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[1-(3-hydroxyphenyl)propan-2-yl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   ethyl    N-[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]-beta-alaninate;-   ethyl    4-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoate;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoate;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-4-methylpentanoate;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2,2-dimethylpropanoate;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}cyclobutanecarboxylic    acid;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2-methylpropanoate;-   2-{(4-cyanobenzyl)[(3-methoxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoic    acid;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-4-methylpentanoic    acid;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2,2-dimethylpropanoic    acid;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2-methylpropanoic    acid;-   N-[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]-beta-alanine;-   4-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoic    acid;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydrofuran-2-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydrofuran-3-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(3-methoxypropanoyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(3-methoxypropyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(tetrahydro-2H-pyran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(tetrahydrofuran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(propan-2-yloxy)ethyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[2-(1,3-dioxolan-2-yl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(1,4-dioxan-2-ylmethyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[3-(4-fluorophenyl)propanoyl](2-methoxyethyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(2-methoxyethyl)[3-(pyridin-3-yl)propanoyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(pyridin-3-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(naphthalen-2-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(2-methoxyethyl)[(4-phenoxyphenyl)acetyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[(4-cyanophenyl)acetyl](2-methoxyethyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(4-aminophenyl)acetyl](2-methoxyethyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{2-[di(prop-2-en-1-yl)amino]ethyl}(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[3-(diethylamino)propyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(diethylamino)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-(pyrrolidin-1-yl)propyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[(1-ethyl-5-oxopyrrolidin-3-yl)methyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(5-oxopyrrolidin-2-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-oxo-3-(pyrrolidin-1-yl)propyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-oxo-2-(piperidin-1-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-(2-oxopyrrolidin-1-yl)propyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(2-oxo-1,3-oxazolidin-3-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl){2-[(2-methylpropanoyl)amino]ethyl}amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-(methylamino)-3-oxopropyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[3-(acetylamino)propyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-oxo-2-(pyrrolidin-1-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   2-[3-(2-hydroxyethyl)-2-oxoimidazolidin-1-yl]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[3-(4-fluorophenyl)-2-oxoimidazolidin-1-yl]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(5-chloropyridin-2-yl)methyl](tetrahydro-2H-pyran-4-ylcarbonyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(5-chloropyridin-2-yl)methyl](tetrahydrofuran-3-ylcarbonyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(5-chloropyridin-2-yl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(5-chloropyridin-2-yl)ethyl](tetrahydrofuran-3-ylcarbonyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(5-chloropyridin-2-yl)ethyl][(2-methoxyethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-([2-(5-chloropyridin-2-yl)ethyl]{[2-(propan-2-yloxy)ethyl]carbamoyl}amino)-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(1,3-benzodioxol-5-ylacetyl)(2-methoxyethyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(5S)-5-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-2-oxo-1,3-oxazolidin-3-yl}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(pyridin-2-ylacetyl)amino]-1,3-thiazole-5-carboxamide;    and pharmaceutically acceptable salts thereof.

Embodiments of Formula (III)

In another aspect, the present invention provides compounds of Formula(III)

and pharmaceutically acceptable salts thereof; wherein each R⁶ is asdescribed herein for Formula (I).

One embodiment of this invention pertains to compounds of Formula (III)or pharmaceutically acceptable salts thereof;

wherein

R⁶, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁶ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR⁸, OR⁸, SR⁸, S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂,NHR⁸, N(R⁸)₂, NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸,NR⁸C(O)OR⁸, NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸,NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸,C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein the aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl represented by R⁶ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁸ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰,OC(O)OR¹⁰, NH₂, NHR¹⁰, N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰,NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰, NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰,NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰, NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰,C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰, C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂,SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂,CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁸ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹, C(O)R¹¹,CO(O)R¹¹, OC(O)R¹¹, OC(O)OR¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹,NR¹¹C(O)R¹¹, NHS(O)₂R¹¹, NR¹¹S(O)₂R¹¹, NHC(O)OR¹¹, NR¹¹C(O)OR¹¹,NHC(O)NH₂, NHC(O)NHR¹¹, NHC(O)N(R¹¹)₂, NR¹¹C(O)NHR¹¹, NR¹¹C(O)N(R¹¹)₂,C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)NHOH, C(O)NHOR¹¹, C(O)NHSO₂R¹¹,C(O)NR¹¹SO₂R¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹¹, C(N)N(R¹¹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁹, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁹ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹², OR¹², SR¹², S(O)R¹², SO₂R¹², C(O)R¹², CO(O)R¹², OC(O)R¹²,OC(O)OR¹², NH₂, NHR¹², N(R¹²)₂, NHC(O)R¹², NR¹²C(O)R¹², NHS(O)₂R¹²,NR¹²S(O)₂R¹², NHC(O)OR¹², NR¹²C(O)OR¹², NHC(O)NH₂, NHC(O)NHR¹²,NHC(O)N(R¹²)₂, NR¹²C(O)NHR¹², NR¹²C(O)N(R¹²)₂, C(O)NH₂, C(O)NHR¹²,C(O)N(R¹²)₂, C(O)NHOH, C(O)NHOR¹², C(O)NHSO₂R¹², C(O)NR¹²SO₂R¹², SO₂NH₂,SO₂NHR¹², SO₂N(R¹²)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR¹², C(N)N(R¹²)₂,CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁹ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³,CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³,NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³,NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂,C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³,C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹³, C(N)N(R¹³)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl,and C₁₋₆ hydroxyalkyl;

R¹¹, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R¹¹ are each independently optionally substituted withone or more substituents independently selected from the groupconsisting of C₁₋₆ alkoxy, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I; wherein the aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl representedby R¹¹ are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of NH₂,C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;

R¹², at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R¹² are each independently optionally substituted withone or more substituents independently selected from the groupconsisting of C₁₋₆ alkoxy, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I; wherein the aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl representedby R¹² are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of NH₂,C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I; and

R¹³, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl; wherein theC₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl represented by R¹³ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of alkoxy, NH₂, C(O)H,C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I.

In another embodiment of Formula (III), R⁶, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R⁶ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R⁸, OR⁸, SR⁸, S(O)R⁸, SO₂R⁸,C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂, NHC(O)R⁸,NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸, NHC(O)NH₂,NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸,C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂,SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁸, C(N)N(R⁸)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁶ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹,OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹,NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂,NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH,C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I. In another embodiment of Formula (III), R⁶, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl, C₂₋₆ alkenyl, aryl, heterocycloalkyl, heteroaryl, and cycloalkyl;wherein the C₁₋₆ alkyl, and C₂₋₆ alkenyl represented by R⁶ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁸, OR⁸, C(O)R⁸,CO(O)R⁸, OC(O)R⁸, N(R⁸)₂, NHC(O)R⁸, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂,C(O)OH, and OH; wherein the aryl, heterocycloalkyl, heteroaryl, andcycloalkyl represented by R⁶ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R⁹, OR⁹, C(O)NH₂, C(O)OH, OH, CN, F, Cl, Br andI.

In one embodiment of Formula (III), R⁸, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R⁸ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰,C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰, N(R¹⁰)₂, NHC(O)R¹⁰,NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰, NR¹⁰C(O)OR¹⁰,NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰, NR¹⁰C(O)N(R¹⁰)₂,C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰, C(O)NHSO₂R¹⁰,C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁸ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹,C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, OC(O)OR¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹,NR¹¹C(O)R¹¹, NHS(O)₂R¹¹, NR¹¹S(O)₂R¹¹, NHC(O)OR¹¹, NR¹¹C(O)OR¹¹,NHC(O)NH₂, NHC(O)NHR¹¹, NHC(O)N(R¹¹)₂, NR¹¹C(O)NHR¹¹, NR¹¹C(O)N(R¹¹)₂,C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)NHOH, C(O)NHOR¹¹, C(O)NHSO₂R¹¹,C(O)NR¹¹SO₂R¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹¹, C(N)N(R¹¹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (III), R⁸, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl, andcycloalkyl; wherein the C₁₋₆ alkyl and C₂₋₆ alkenyl represented by R⁸are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of OH, F,Cl, Br and I; wherein the aryl, heterocycloalkyl, and heteroarylrepresented by R⁸ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹¹, OR¹¹, NH₂, N(R¹¹)₂, C(O)H, OH, CN, F, Cl, Br and I.

In one embodiment of Formula (III), R⁹, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R⁹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹², OR¹², SR¹², S(O)R¹², SO₂R¹²,C(O)R¹², CO(O)R¹², OC(O)R¹², OC(O)OR¹², NH₂, NHR¹², N(R¹²)₂, NHC(O)R¹²,NR¹²C(O)R¹², NHS(O)₂R¹², NR¹²S(O)₂R¹², NHC(O)OR¹², NR¹²C(O)OR¹²,NHC(O)NH₂, NHC(O)NHR¹², NHC(O)N(R¹²)₂, NR¹²C(O)NHR¹², NR¹²C(O)N(R¹²)₂,C(O)NH₂, C(O)NHR¹², C(O)N(R¹²)₂, C(O)NHOH, C(O)NHOR¹², C(O)NHSO₂R¹²,C(O)NR¹²SO₂R¹², SO₂NH₂, SO₂NHR¹², SO₂N(R¹²)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹², C(N)N(R¹²)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³,C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³,NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³,NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂,C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³,C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹³, C(N)N(R¹³)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (III), R⁹, at each occurrence, is C₁₋₆alkyl.

In one embodiment of Formula (III), R¹⁰, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, and C₁₋₆ hydroxyalkyl.

In one embodiment of Formula (III), R¹¹, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R¹¹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of C₁₋₆ alkoxy, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R¹¹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I. In another embodiment of Formula (III), R¹¹, ateach occurrence, is independently selected from the group consisting ofC₁₋₆ alkyl, C₂₋₆ alkenyl, aryl, and heteroaryl; wherein the C₁₋₆ alkyland C₂₋₆ alkenyl represented by R¹¹ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of C₁₋₆ alkoxy, cycloalkyl, OH, F, Cl, Br and I.

In one embodiment of Formula (III), R¹², at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R¹² are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of C₁₋₆ alkoxy, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R¹² are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I.

In one embodiment of Formula (III), R¹³, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, andC₂₋₆ alkynyl represented by R¹³ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of alkoxy, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F,Cl, Br and I.

In another embodiment of Formula (III), R⁶, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, aryl,heterocycloalkyl, heteroaryl, and cycloalkyl; wherein the C₁₋₆ alkylrepresented by R⁶ is independently optionally substituted with one ormore substituents independently selected from the group consisting ofR⁸, OR⁸, C(O)R⁸, OC(O)R⁸, N(R⁸)₂, NHC(O)R⁸, C(O)NHR⁸, and OH; whereinthe aryl, heterocycloalkyl, and heteroaryl represented by R⁶ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁹, OR⁹, C(O)NH₂,OH, CN, F, Cl, Br and I. In another embodiment of Formula (III), R⁸, ateach occurrence, is independently selected from the group consisting ofC₁₋₆ alkyl, C₂₋₆ alkenyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, and cycloalkyl; wherein the aryl, heterocycloalkyl, andheteroaryl represented by R⁸ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹¹, OR¹¹, NH₂, N(R¹¹)₂, C(O)H, OH, CN, F, Cl,Br and I. In another embodiment of Formula (III), R⁹, at eachoccurrence, is C₁₋₆ alkyl. In another embodiment of Formula (III), R¹¹,at each occurrence, is independently selected from the group consistingof C₁₋₆ alkyl, C₂₋₆ alkenyl, and aryl; wherein the C₁₋₆ alkyl and C₂₋₆alkenyl represented by R¹¹ are each independently optionally substitutedwith one or more substituents independently selected from the groupconsisting of C₁₋₆ alkoxy, cycloalkyl, OH, F, Cl, Br and I.

Still another embodiment pertains to compounds having Formula (III),which include

-   2-[(4-fluorobenzyl)(tetrahydro-2H-pyran-4-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(cyclohexylacetyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(3-methylbutanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzoyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(3-chlorobenzoyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzoyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(methoxyacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(N,N-dimethylglycyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(3,6-dihydropyridin-1(2H)-ylacetyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(4-methylpiperidin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(4-hydroxypiperidin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(4-methylpiperazin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[4-(propan-2-yl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(4-formylpiperazin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(hexahydropyrrolo[1,2-a]pyrazin-2(1H)-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[4-(cyclopropylmethyl)piperazin-1-yl]acetyl}(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[4-(2-ethoxyethyl)piperazin-1-yl]acetyl}(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(cyclopropylcarbonyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[4-(prop-2-en-1-yl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[4-(3-methoxypropyl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[3-(dimethylamino)pyrrolidin-1-yl]acetyl}(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(morpholin-4-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(3-hydroxypiperidin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[4-(2-hydroxyethyl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(1,4-dioxa-7-azaspiro[4.4]non-7-ylacetyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   1-{2-[(4-fluorobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)amino]-2-oxoethyl}pyridinium;-   2-{[2-(4-fluorophenyl)ethyl](3-methylbutanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(4-cyanophenyl)ethyl](3-methylbutanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(4-cyanophenyl)ethyl](tetrahydro-2H-pyran-4-ylacetyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methylbutanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(tetrahydro-2H-pyran-4-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(4-cyanophenyl)ethyl](tetrahydrofuran-3-ylacetyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(tetrahydrofuran-3-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N¹-(4-fluorobenzyl)-N¹-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)piperidine-1,3-dicarboxamide;-   2-{(4-fluorobenzyl)[(3-hydroxyazetidin-1-yl)carbonyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-1,4-dioxa-7-azaspiro[4.4]nonane-7-carboxamide;-   2-{(4-fluorobenzyl)[(3-methoxypyrrolidin-1-yl)carbonyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-2,6-dimethylmorpholine-4-carboxamide;-   N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-2,2-dimethylmorpholine-4-carboxamide;-   N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-1,4-oxazepane-4-carboxamide;-   2-[(4-fluorobenzoyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(4-methylbenzyl)amino]-1,3-thiazole-5-carboxamide;-   N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-N-(3-methylbutyl)-1,2-oxazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(2-phenoxypropanoyl)amino]-1,3-thiazole-5-carboxamide;-   2-{[2-(4-cyanophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(pyrimidin-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(2-methoxypyridin-4-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(1,3-oxazol-4-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   2-{[(5-chloropyridin-2-yl)methyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(4-methylpyridin-3-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(6-methoxypyridin-3-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(4-methyl-1,3-thiazol-5-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[2-(3-hydroxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(pyridin-2-yl)ethyl]amino}-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(1,3-benzodioxol-5-yl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(4-chlorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(3-fluorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(4-hydroxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(3-chlorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   N-[3-(1H-imidazol-1-yl)propyl]-2-{[2-(3-methoxyphenyl)ethyl](3-methoxypropanoyl)amino}-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-(2-fluorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   2-{[2-hydroxy-2-(4-methoxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide    acetate (1:1);-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[1-(pyridin-2-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(1-methyl-1H-pyrazol-4-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(2,6-difluorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(6-methylpyridin-3-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(4-chlorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(5-methylpyrazin-2-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(3-chlorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(5-methylpyridin-2-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(2,5-difluorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(2-methylbenzyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(3-methylbenzyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(pyridin-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(pyridin-3-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methylbutyl)[(2R)-2-phenoxypropanoyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methylbutyl)[(2S)-2-phenoxypropanoyl]amino}-1,3-thiazole-5-carboxamide;-   N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-5-methyl-N-(3-methylbutyl)-1,2-oxazole-3-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(phenoxyacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(3-phenylpropanoyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(2-phenylpropanoyl)amino]-1,3-thiazole-5-carboxamide;-   2-{[(4-fluorophenyl)acetyl](3-methylbutyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(3-methylbutyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(methoxyacetyl)(3-methylbutyl)amino]-1,3-thiazole-5-carboxamide;-   2-[(cyclopropylcarbonyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   (2S)-1-[(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)(3-methylbutyl)amino]-1-oxopropan-2-yl    acetate;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydro-2H-pyran-4-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydrofuran-3-ylcarbonyl)amino]-1,3-thiazole-5-carboxamide;-   2-{[2-hydroxy-2-(3-methoxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(pyrazin-2-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[1-(3-hydroxyphenyl)propan-2-yl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydrofuran-2-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydrofuran-3-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(3-methoxypropanoyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(3-methoxypropyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(tetrahydro-2H-pyran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(tetrahydrofuran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(propan-2-yloxy)ethyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[2-(1,3-dioxolan-2-yl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(1,4-dioxan-2-ylmethyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[3-(4-fluorophenyl)propanoyl](2-methoxyethyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(2-methoxyethyl)[3-(pyridin-3-yl)propanoyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(pyridin-3-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(naphthalen-2-ylacetyl)amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(2-methoxyethyl)[(4-phenoxyphenyl)acetyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[(4-cyanophenyl)acetyl](2-methoxyethyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(4-aminophenyl)acetyl](2-methoxyethyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{2-[di(prop-2-en-1-yl)amino]ethyl}(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[3-(diethylamino)propyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(diethylamino)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-(pyrrolidin-1-yl)propyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[(1-ethyl-5-oxopyrrolidin-3-yl)methyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(5-oxopyrrolidin-2-yl)methyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-oxo-3-(pyrrolidin-1-yl)propyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-oxo-2-(piperidin-1-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-(2-oxopyrrolidin-1-yl)propyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(2-oxo-1,3-oxazolidin-3-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl){2-[(2-methylpropanoyl)amino]ethyl}amino]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-(methylamino)-3-oxopropyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[3-(acetylamino)propyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-oxo-2-(pyrrolidin-1-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;-   2-{[(5-chloropyridin-2-yl)methyl](tetrahydro-2H-pyran-4-ylcarbonyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(5-chloropyridin-2-yl)methyl](tetrahydrofuran-3-ylcarbonyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(5-chloropyridin-2-yl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(5-chloropyridin-2-yl)ethyl](tetrahydrofuran-3-ylcarbonyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(1,3-benzodioxol-5-ylacetyl)(2-methoxyethyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(pyridin-2-ylacetyl)amino]-1,3-thiazole-5-carboxamide;    and pharmaceutically acceptable salts thereof.

Embodiments of Formula (IV)

In another aspect, the present invention provides compounds of Formula(IV)

and pharmaceutically acceptable salts thereof; wherein each R⁶ is asdescribed herein for Formula (I).

One embodiment of this invention pertains to compounds of Formula (IV)or pharmaceutically acceptable salts thereof;

wherein

R⁶, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁶ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR⁸, OR⁸, SR⁸, S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂,NHR⁸, N(R⁸)₂, NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸,NR⁸C(O)OR⁸, NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸,NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸,C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein the aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl represented by R⁶ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁸ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰,OC(O)OR¹⁰, NH₂, NHR¹⁰, N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰,NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰, NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰,NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰, NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰,C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰, C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂,SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂,CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁸ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹, C(O)R¹¹,CO(O)R¹¹, OC(O)R¹¹, OC(O)OR¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹,NR¹¹C(O)R¹¹, NHS(O)₂R¹¹, NR¹¹S(O)₂R¹¹, NHC(O)OR¹¹, NR¹¹C(O)OR¹¹,NHC(O)NH₂, NHC(O)NHR¹¹, NHC(O)N(R¹¹)₂, NR¹¹C(O)NHR¹¹, NR¹¹C(O)N(R¹¹)₂,C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)NHOH, C(O)NHOR¹¹, C(O)NHSO₂R¹¹,C(O)NR¹¹SO₂R¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹¹, C(N)N(R¹¹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁹, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁹ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹², OR¹², SR¹², S(O)R¹², SO₂R¹², C(O)R¹², CO(O)R¹², OC(O)R¹²,OC(O)OR¹², NH₂, NHR¹², N(R¹²)₂, NHC(O)R¹², NR¹²C(O)R¹², NHS(O)₂R¹²,NR¹²S(O)₂R¹², NHC(O)OR¹², NR¹²C(O)OR¹², NHC(O)NH₂, NHC(O)NHR¹²,NHC(O)N(R¹²)₂, NR¹²C(O)NHR¹², NR¹²C(O)N(R¹²)₂, C(O)NH₂, C(O)NHR¹²,C(O)N(R¹²)₂, C(O)NHOH, C(O)NHOR¹², C(O)NHSO₂R¹², C(O)NR¹²SO₂R¹², SO₂NH₂,SO₂NHR¹², SO₂N(R¹²)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR¹², C(N)N(R¹²)₂,CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁹ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³,CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³,NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³,NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂,C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³,C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹³, C(N)N(R¹³)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl,and C₁₋₆ hydroxyalkyl;

R¹¹, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R¹¹ are each independently optionally substituted withone or more substituents independently selected from the groupconsisting of C₁₋₆ alkoxy, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I; wherein the aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl representedby R¹¹ are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of NH₂,C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;

R¹², at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R¹² are each independently optionally substituted withone or more substituents independently selected from the groupconsisting of C₁₋₆ alkoxy, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I; wherein the aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl representedby R¹² are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of NH₂,C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I; and

R¹³, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl; wherein theC₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl represented by R¹³ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of alkoxy, NH₂, C(O)H,C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I.

In one embodiment of Formula (IV), R⁶, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R⁶ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R⁸, OR⁸, SR⁸, S(O)R⁸, SO₂R⁸,C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂, NHC(O)R⁸,NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸, NHC(O)NH₂,NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸,C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂,SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁸, C(N)N(R⁸)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁶ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹,OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹,NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂,NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH,C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I. In another embodiment of Formula (IV), R⁶, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl, C₂₋₆ alkenyl, aryl, heterocycloalkyl, heteroaryl, and cycloalkyl;wherein the C₁₋₆ alkyl, and C₂₋₆ alkenyl represented by R⁶ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁸, OR⁸, C(O)R⁸,CO(O)R⁸, OC(O)R⁸, N(R⁸)₂, NHC(O)R⁸, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂,C(O)OH, and OH; wherein the aryl, heterocycloalkyl, heteroaryl, andcycloalkyl represented by R⁶ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R⁹, OR⁹, C(O)NH₂, C(O)OH, OH, CN, F, Cl, Br andI.

In one embodiment of Formula (IV), R⁸, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R⁸ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰,C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰, N(R¹⁰)₂, NHC(O)R¹⁰,NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰, NR¹⁰C(O)OR¹⁰,NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰, NR¹⁰C(O)N(R¹⁰)₂,C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰, C(O)NHSO₂R¹⁰,C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁸ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹,C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, OC(O)OR¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹,NR¹¹C(O)R¹¹, NHS(O)₂R¹¹, NR¹¹S(O)₂R¹¹, NHC(O)OR¹¹, NR¹¹C(O)OR¹¹,NHC(O)NH₂, NHC(O)NHR¹¹, NHC(O)N(R¹¹)₂, NR¹¹C(O)NHR¹¹, NR¹¹C(O)N(R¹¹)₂,C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)NHOH, C(O)NHOR¹¹, C(O)NHSO₂R¹¹,C(O)NR¹¹SO₂R¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹¹, C(N)N(R¹¹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (IV), R⁸, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl, andcycloalkyl; wherein the C₁₋₆ alkyl and C₂₋₆ alkenyl represented by R⁸are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of OH, F,Cl, Br and I; wherein the aryl, heterocycloalkyl, and heteroarylrepresented by R⁸ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹¹, OR¹¹, NH₂, N(R¹¹)₂, C(O)H, OH, CN, F, Cl, Br and I.

In one embodiment of Formula (IV), R⁹, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R⁹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹², OR¹², SR¹², S(O)R¹², SO₂R¹²,C(O)R¹², CO(O)R¹², OC(O)R¹², OC(O)OR¹², NH₂, NHR¹², N(R¹²)₂, NHC(O)R¹²,NR¹²C(O)R¹², NHS(O)₂R¹², NR¹²S(O)₂R¹², NHC(O)OR¹², NR¹²C(O)OR¹²,NHC(O)NH₂, NHC(O)NHR¹², NHC(O)N(R¹²)₂, NR¹²C(O)NHR¹², NR¹²C(O)N(R¹²)₂,C(O)NH₂, C(O)NHR¹², C(O)N(R¹²)₂, C(O)NHOH, C(O)NHOR¹², C(O)NHSO₂R¹²,C(O)NR¹²SO₂R¹², SO₂NH₂, SO₂NHR¹², SO₂N(R¹²)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹², C(N)N(R¹²)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³,C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³,NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³,NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂,C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³,C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹³, C(N)N(R¹³)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (IV), R⁹, at each occurrence, is C₁₋₆alkyl.

In one embodiment of Formula (IV), R¹⁰, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, and C₁₋₆ hydroxyalkyl.

In one embodiment of Formula (IV), R¹¹, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R¹¹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of C₁₋₆ alkoxy, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R¹¹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I. In another embodiment of Formula (IV), R¹¹, ateach occurrence, is independently selected from the group consisting ofC₁₋₆ alkyl, C₂₋₆ alkenyl, aryl, and heteroaryl; wherein the C₁₋₆ alkyland C₂₋₆ alkenyl represented by R¹¹ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of C₁₋₆ alkoxy, cycloalkyl, OH, F, Cl, Br and I.

In one embodiment of Formula (IV), R¹², at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R¹² are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of C₁₋₆ alkoxy, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R¹² are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I.

In one embodiment of Formula (IV), R¹³, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, andC₂₋₆ alkynyl represented by R¹³ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of alkoxy, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F,Cl, Br and I.

In another embodiment of Formula (IV), R⁶, at each occurrence, is C₁₋₆alkyl; wherein the C₁₋₆ alkyl represented by R⁶ is independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R⁸, C(O)R⁸, C(O)NHR⁸, andC(O)N(R⁸)₂. In another embodiment of Formula (IV), R⁸, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl, aryl, and heterocycloalkyl; wherein the aryl, andheterocycloalkyl represented by R⁸ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹¹, CN, F, Cl, Br and I. In another embodimentof Formula (IV), R¹¹, at each occurrence, is independently selected fromthe group consisting of C₁₋₆ alkyl and heteroaryl.

Still another embodiment pertains to compounds having Formula (IV),which include

-   2-{(4-fluorobenzyl)[4-(pyridin-3-yl)benzyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   N-[3-(1H-imidazol-1-yl)propyl]-2-{methyl[4-(pyridin-3-yl)benzyl]amino}-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(methyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[3-(morpholin-4-yl)propyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[3-(piperidin-1-yl)propyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[2-(pyrrolidin-1-yl)ethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){2-[4-(propan-2-yl)piperazin-1-yl]ethyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(5-chloro-1,3-benzodioxol-4-yl)methyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-chlorobenzyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(2-chlorobenzyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(2,5-dichlorobenzyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[2-(methylamino)-2-oxoethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[2-oxo-2-(propan-2-ylamino)ethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(dimethylamino)-2-oxoethyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[2-(diethylamino)-2-oxoethyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[2-(morpholin-4-yl)-2-oxoethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(4-methylbenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(2-fluorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(3-fluorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(2-chlorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(3-chlorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-chlorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;    and pharmaceutically acceptable salts thereof.

Embodiments of Formula (V)

In another aspect, the present invention provides compounds of Formula(V)

and pharmaceutically acceptable salts thereof; wherein each R⁶ is asdescribed herein for Formula (I).

One embodiment of this invention pertains to compounds of Formula (V) orpharmaceutically acceptable salts thereof;

wherein

R⁶, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁶ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR⁸, OR⁸, SR⁸, S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂,NHR⁸, N(R⁸)₂, NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸,NR⁸C(O)OR⁸, NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸,NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸,C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein the aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl represented by R⁶ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁸ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰,OC(O)OR¹⁰, NH₂, NHR¹⁰, N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰,NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰, NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰,NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰, NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰,C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰, C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂,SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂,CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁸ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹, C(O)R¹¹,CO(O)R¹¹, OC(O)R¹¹, OC(O)OR¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹,NR¹¹C(O)R¹¹, NHS(O)₂R¹¹, NR¹¹S(O)₂R¹¹, NHC(O)OR¹¹, NR¹¹C(O)OR¹¹,NHC(O)NH₂, NHC(O)NHR¹¹, NHC(O)N(R¹¹)₂, NR¹¹C(O)NHR¹¹, NR¹¹C(O)N(R¹¹)₂,C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)NHOH, C(O)NHOR¹¹, C(O)NHSO₂R¹¹,C(O)NR¹¹SO₂R¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹¹, C(N)N(R¹¹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁹, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁹ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹², OR¹², SR¹², S(O)R¹², SO₂R¹², C(O)R¹², CO(O)R¹², OC(O)R¹²,OC(O)OR¹², NH₂, NHR¹², N(R¹²)₂, NHC(O)R¹², NR¹²C(O)R¹², NHS(O)₂R¹²,NR¹²S(O)₂R¹², NHC(O)OR¹², NR¹²C(O)OR¹², NHC(O)NH₂, NHC(O)NHR¹²,NHC(O)N(R¹²)₂, NR¹²C(O)NHR¹², NR¹²C(O)N(R¹²)₂, C(O)NH₂, C(O)NHR¹²,C(O)N(R¹²)₂, C(O)NHOH, C(O)NHOR¹², C(O)NHSO₂R¹², C(O)NR¹²SO₂R¹², SO₂NH₂,SO₂NHR¹², SO₂N(R¹²)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR¹², C(N)N(R¹²)₂,CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁹ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³,CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³,NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³,NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂,C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³,C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹³, C(N)N(R¹³)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl,and C₁₋₆ hydroxyalkyl;

R¹¹, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R¹¹ are each independently optionally substituted withone or more substituents independently selected from the groupconsisting of C₁₋₆ alkoxy, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I; wherein the aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl representedby R¹¹ are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of NH₂,C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;

R¹², at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R¹² are each independently optionally substituted withone or more substituents independently selected from the groupconsisting of C₁₋₆ alkoxy, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I; wherein the aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl representedby R¹² are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of NH₂,C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I; and

R¹³, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl; wherein theC₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl represented by R¹³ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of alkoxy, NH₂, C(O)H,C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I.

In one embodiment of Formula (V), R⁶, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R⁶ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R⁸, OR⁸, SR⁸, S(O)R⁸, SO₂R⁸,C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂, NHC(O)R⁸,NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸, NHC(O)NH₂,NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸,C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂,SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁸, C(N)N(R⁸)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁶ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹,OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹,NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂,NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH,C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I. In another embodiment of Formula (V), R⁶, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl, C₂₋₆ alkenyl, aryl, heterocycloalkyl, heteroaryl, and cycloalkyl;wherein the C₁₋₆ alkyl, and C₂₋₆ alkenyl represented by R⁶ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁸, OR⁸, C(O)R⁸,CO(O)R⁸, OC(O)R⁸, N(R⁸)₂, NHC(O)R⁸, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂,C(O)OH, and OH; wherein the aryl, heterocycloalkyl, heteroaryl, andcycloalkyl represented by R⁶ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R⁹, OR⁹, C(O)NH₂, C(O)OH, OH, CN, F, Cl, Br andI.

In one embodiment of Formula (V), R⁸, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R⁸ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰,C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰, N(R¹⁰)₂, NHC(O)R¹⁰,NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰, NR¹⁰C(O)OR¹⁰,NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰, NR¹⁰C(O)N(R¹⁰)₂,C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰, C(O)NHSO₂R¹⁰,C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁸ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹,C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, OC(O)OR¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹,NR¹¹C(O)R¹¹, NHS(O)₂R¹¹, NR¹¹S(O)₂R¹¹, NHC(O)OR¹¹, NR¹¹C(O)OR¹¹,NHC(O)NH₂, NHC(O)NHR¹¹, NHC(O)N(R¹¹)₂, NR¹¹C(O)NHR¹¹, NR¹¹C(O)N(R¹¹)₂,C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)NHOH, C(O)NHOR¹¹, C(O)NHSO₂R¹¹,C(O)NR¹¹SO₂R¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹¹, C(N)N(R¹¹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (V), R⁸, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl, andcycloalkyl; wherein the C₁₋₆ alkyl and C₂₋₆ alkenyl represented by R⁸are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of OH, F,Cl, Br and I; wherein the aryl, heterocycloalkyl, and heteroarylrepresented by R⁸ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹¹, OR¹¹, NH₂, N(R¹¹)₂, C(O)H, OH, CN, F, Cl, Br and I.

In one embodiment of Formula (V), R⁹, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R⁹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹², OR¹², SR¹², S(O)R¹², SO₂R¹²,C(O)R¹², CO(O)R¹², OC(O)R¹², OC(O)OR¹², NH₂, NHR¹², N(R¹²)₂, NHC(O)R¹²,NR¹²C(O)R¹², NHS(O)₂R¹², NR¹²S(O)₂R¹², NHC(O)OR¹², NR¹²C(O)OR¹²,NHC(O)NH₂, NHC(O)NHR¹², NHC(O)N(R¹²)₂, NR¹²C(O)NHR¹², NR¹²C(O)N(R¹²)₂,C(O)NH₂, C(O)NHR¹², C(O)N(R¹²)₂, C(O)NHOH, C(O)NHOR¹², C(O)NHSO₂R¹²,C(O)NR¹²SO₂R¹², SO₂NH₂, SO₂NHR¹², SO₂N(R¹²)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹², C(N)N(R¹²)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³,C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³,NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³,NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂,C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³,C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹³, C(N)N(R¹³)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (V), R⁹, at each occurrence, is C₁₋₆alkyl.

In one embodiment of Formula (V), R¹⁰, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, and C₁₋₆ hydroxyalkyl.

In one embodiment of Formula (V), R¹¹, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R¹¹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of C₁₋₆ alkoxy, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R¹¹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I. In another embodiment of Formula (V), R¹¹, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl, C₂₋₆ alkenyl, aryl, and heteroaryl; wherein the C₁₋₆ alkyl andC₂₋₆ alkenyl represented by R¹¹ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of C₁₋₆ alkoxy, cycloalkyl, OH, F, Cl, Br and I.

In one embodiment of Formula (V), R¹², at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R¹² are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of C₁₋₆ alkoxy, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R¹² are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I.

In one embodiment of Formula (V), R¹³, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, andC₂₋₆ alkynyl represented by R¹³ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of alkoxy, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F,Cl, Br and I.

In another embodiment of Formula (V), R⁶, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, heterocycloalkyl, and cycloalkyl; wherein the C₁₋₆ alkyl andC₂₋₆ alkenyl represented by R⁶ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R⁸, OR⁸, C(O)OR⁸, N(R⁸)₂, NHC(O)R⁸, C(O)NH₂,C(O)N(R⁸)₂, C(O)OH, and OH; wherein the heterocycloalkyl, and cycloalkylrepresented by R⁶ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofC(O)NH₂, C(O)OH, F, Cl, Br and I. In another embodiment of Formula (V),R⁸, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, aryl, heterocycloalkyl, and heteroaryl;wherein the C₁₋₆ alkyl is independently optionally substituted with oneor more OH; wherein the aryl, heterocycloalkyl, and heteroarylrepresented by R⁸ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofOH, CN, F, Cl, Br and I.

Still another embodiment pertains to compounds having Formula (V), whichinclude

-   2-[(4-fluorobenzyl)(propan-2-ylcarbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(3-methylbutyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-methylpropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-propoxyethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(tetrahydrofuran-2-ylmethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(1-methoxypropan-2-yl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-methoxyethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(2-ethoxyethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(1-methoxybutan-2-yl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(1,3-dioxolan-2-ylmethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[2-(propan-2-yloxy)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(1,4-dioxan-2-ylmethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(1,3-dimethoxypropan-2-yl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-methoxybutyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(tetrahydrofuran-3-ylcarbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(tetrahydro-2H-pyran-3-ylcarbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[2-(propan-2-yloxy)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(2-methoxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[2-(2-hydroxyethoxy)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(propan-2-yloxy)propyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(3-hydroxy-2,2-dimethylpropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(2-hydroxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(1-hydroxypropan-2-yl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(3-hydroxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[(2S)-1-hydroxybut-3-en-2-yl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(4-hydroxybutyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(3-amino-3-oxopropyl)carbamoyl](4-cyanobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[3-(acetylamino)-2-methylpropyl]carbamoyl}(4-cyanobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(dimethylamino)-3-oxopropyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(3-ethoxy-2-hydroxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(diethylamino)propyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[2-(acetylamino)ethyl]carbamoyl}(4-cyanobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[2-(diethylamino)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)({2-[(2-methylpropanoyl)amino]ethyl}carbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[(2R)-1-hydroxybut-3-en-2-yl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(3-hydroxyazetidin-1-yl)propyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   ethyl    N-[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]-beta-alaninate;-   ethyl    4-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoate;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoate;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-4-methylpentanoate;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2,2-dimethylpropanoate;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}cyclobutanecarboxylic    acid;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2-methylpropanoate;-   2-{(4-cyanobenzyl)[(3-methoxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoic    acid;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-4-methylpentanoic    acid;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2,2-dimethylpropanoic    acid;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2-methylpropanoic    acid;-   N-[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]-beta-alanine;-   4-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoic    acid;-   2-{[2-(5-chloropyridin-2-yl)ethyl][(2-methoxyethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-([2-(5-chloropyridin-2-yl)ethyl]{[2-(propan-2-yloxy)ethyl]carbamoyl}amino)-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;    and pharmaceutically acceptable salts thereof.

Embodiments of Formula (VI)

In another aspect, the present invention provides compounds of Formula(VI)

and pharmaceutically acceptable salts thereof; wherein each R⁶ is asdescribed herein for Formula (I), and R^(x) is as described herein forsubstituents on R⁸ when R⁸ is aryl.

One embodiment of this invention pertains to compounds of Formula (VI)or pharmaceutically acceptable salts thereof;

wherein

R⁶, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁶ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR⁸, OR⁸, SR⁸, S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂,NHR⁸, N(R⁸)₂, NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸,NR⁸C(O)OR⁸, NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸,NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸,C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein the aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl represented by R⁶ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁸, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁸ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹⁰, OR¹⁰, Se, S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰,NH₂, NHR¹⁰, N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰,NHC(O)OR¹⁰, NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂,NR¹⁰C(O)NHR¹⁰, NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂,C(O)NHOH, C(O)NHOR¹⁰, C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰,SO₂N(R¹⁰)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁸ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹, C(O)R¹¹,CO(O)R¹¹, OC(O)R¹¹, OC(O)OR¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹,NR¹¹C(O)R¹¹, NHS(O)₂R¹¹, NR¹¹S(O)₂R¹¹, NHC(O)OR¹¹, NR¹¹C(O)OR¹¹,NHC(O)NH₂, NHC(O)NHR¹¹, NHC(O)N(R¹¹)₂, NR¹¹C(O)NHR¹¹, NR¹¹C(O)N(R¹¹)₂,C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)NHOH, C(O)NHOR¹¹, C(O)NHSO₂R¹¹,C(O)NR¹¹SO₂R¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹¹, C(N)N(R¹¹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R^(x) is independently selected from the group consisting of R¹¹, OR¹¹,SR¹¹, S(O)R¹¹, SO₂R¹¹, C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, OC(O)OR¹¹, NH₂,NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹, NR¹¹C(O)R¹¹, NHS(O)₂R¹¹, NR¹¹S(O)₂R¹¹,NHC(O)OR¹¹, NR¹¹C(O)OR¹¹, NHC(O)NH₂, NHC(O)NHR¹¹, NHC(O)N(R¹¹)₂,NR¹¹C(O)NHR¹¹, NR¹¹C(O)N(R¹¹)₂, C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂,C(O)NHOH, C(O)NHOR¹¹, C(O)NHSO₂R¹¹, C(O)NR¹¹SO₂R¹¹, SO₂NH₂, SO₂NHR¹¹,SO₂N(R¹¹)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR¹¹, C(N)N(R¹¹)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R⁹, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁹ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹², OR¹², SR¹², S(O)R¹², SO₂R¹², C(O)R¹², CO(O)R¹², OC(O)R¹²,OC(O)OR¹², NH₂, NHR¹², N(R¹²)₂, NHC(O)R¹², NR¹²C(O)R¹², NHS(O)₂R¹²,NR¹²S(O)₂R¹², NHC(O)OR¹², NR¹²C(O)OR¹², NHC(O)NH₂, NHC(O)NHR¹²,NHC(O)N(R¹²)₂, NR¹²C(O)NHR¹², NR¹²C(O)N(R¹²)₂, C(O)NH₂, C(O)NHR¹²,C(O)N(R¹²)₂, C(O)NHOH, C(O)NHOR¹², C(O)NHSO₂R¹², C(O)NR¹²SO₂R¹², SO₂NH₂,SO₂NHR¹², SO₂N(R¹²)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR¹², C(N)N(R¹²)₂,CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁹ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³,CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³,NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³,NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂,C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³,C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹³, C(N)N(R¹³)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;

R¹⁰, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl,and C₁₋₆ hydroxyalkyl;

R¹¹, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R¹¹ are each independently optionally substituted withone or more substituents independently selected from the groupconsisting of C₁₋₆ alkoxy, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I; wherein the aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl representedby R¹¹ are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of NH₂,C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;

R¹², at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R¹² are each independently optionally substituted withone or more substituents independently selected from the groupconsisting of C₁₋₆ alkoxy, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I; wherein the aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl representedby R¹² are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of NH₂,C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I; and

R¹³, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl; wherein theC₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl represented by R¹³ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of alkoxy, NH₂, C(O)H,C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I.

In one embodiment of Formula (IV), R⁶ is independently selected from thegroup consisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁶ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR⁸, OR⁸, SR⁸, S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂,NHR⁸, N(R⁸)₂, NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸,NR⁸C(O)OR⁸, NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸,NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸,C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein the aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl represented by R⁶ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I. Inanother embodiment of Formula (IV), R⁶ is independently selected fromthe group consisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, aryl,heterocycloalkyl, heteroaryl, and cycloalkyl; wherein the C₁₋₆ alkyl,and C₂₋₆ alkenyl represented by R⁶ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R⁸, OR⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, N(R⁸)₂,NHC(O)R⁸, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)OH, and OH; wherein thearyl, heterocycloalkyl, heteroaryl, and cycloalkyl represented by R⁶ areeach independently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁹, OR⁹, C(O)NH₂,C(O)OH, OH, CN, F, Cl, Br and I.

In one embodiment of Formula (IV), R⁸, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R⁸ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰,C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰, OC(O)OR¹⁰, NH₂, NHR¹⁰, N(R¹⁰)₂, NHC(O)R¹⁰,NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰, NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰, NR¹⁰C(O)OR¹⁰,NHC(O)NH₂, NHC(O)NHR¹⁰, NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰, NR¹⁰C(O)N(R¹⁰)₂,C(O)NH₂, C(O)NHR¹⁰, C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰, C(O)NHSO₂R¹⁰,C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂, SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹⁰, C(N)N(R¹⁰)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁸ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹,C(O)R¹¹, CO(O)R¹¹, OC(O)R¹¹, OC(O)OR¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹,NR¹¹C(O)R¹¹, NHS(O)₂R¹¹, NR¹¹S(O)₂R¹¹, NHC(O)OR¹¹, NR¹¹C(O)OR¹¹,NHC(O)NH₂, NHC(O)NHR¹¹, NHC(O)N(R¹¹)₂, NR¹¹C(O)NHR¹¹, NR¹¹C(O)N(R¹¹)₂,C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)NHOH, C(O)NHOR¹¹, C(O)NHSO₂R¹¹,C(O)NR¹¹SO₂R¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹¹, C(N)N(R¹¹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (IV), R⁸, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl, andcycloalkyl; wherein the C₁₋₆ alkyl and C₂₋₆ alkenyl represented by R⁸are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of OH, F,Cl, Br and I; wherein the aryl, heterocycloalkyl, and heteroarylrepresented by R⁸ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹¹, OR¹¹, NH₂, N(R¹¹)₂, C(O)H, OH, CN, F, Cl, Br and I.

In one embodiment of Formula (IV), R⁹, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R⁹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹², OR¹², SR¹², S(O)R¹², SO₂R¹²,C(O)R¹², CO(O)R¹², OC(O)R¹², OC(O)OR¹², NH₂, NHR¹², N(R¹²)₂, NHC(O)R¹²,NR¹²C(O)R¹², NHS(O)₂R¹², NR¹²S(O)₂R¹², NHC(O)OR¹², NR¹²C(O)OR¹²,NHC(O)NH₂, NHC(O)NHR¹², NHC(O)N(R¹²)₂, NR¹²C(O)NHR¹², NR¹²C(O)N(R¹²)₂,C(O)NH₂, C(O)NHR¹², C(O)N(R¹²)₂, C(O)NHOH, C(O)NHOR¹², C(O)NHSO₂R¹²,C(O)NR¹²SO₂R¹², SO₂NH₂, SO₂NHR¹², SO₂N(R¹²)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹², C(N)N(R¹²)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³,C(O)R¹³, CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³,NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³,NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂,C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³,C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹³, C(N)N(R¹³)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I.In another embodiment of Formula (IV), R⁹, at each occurrence, is C₁₋₆alkyl.

In one embodiment of Formula (IV), R¹⁰, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl, and C₁₋₆ hydroxyalkyl.

In one embodiment of Formula (IV), R¹¹, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R¹¹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of C₁₋₆ alkoxy, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R¹¹ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I. In another embodiment of Formula (IV), R¹¹, ateach occurrence, is independently selected from the group consisting ofC₁₋₆ alkyl, C₂₋₆ alkenyl, aryl, and heteroaryl; wherein the C₁₋₆ alkyland C₂₋₆ alkenyl represented by R¹¹ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of C₁₋₆ alkoxy, cycloalkyl, OH, F, Cl, Br and I.

In one embodiment of Formula (IV), R¹², at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R¹² are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of C₁₋₆ alkoxy, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R¹² are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I.

In one embodiment of Formula (IV), R¹³, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, andC₂₋₆ alkynyl represented by R¹³ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of alkoxy, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F,Cl, Br and I.

In one embodiment of Formula (IV), R⁶ is independently selected from thegroup consisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, heterocycloalkyl, andcycloalkyl; wherein the C₁₋₆ alkyl and C₂₋₆ alkenyl represented by R⁶are independently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁸, OR⁸, C(O)OR⁸,N(R⁸)₂, NHC(O)R⁸, C(O)NH₂, C(O)N(R⁸)₂, C(O)OH, and OH; wherein theheterocycloalkyl, and cycloalkyl represented by R⁶ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of C(O)OH, F, Cl, Brand I. In another embodiment of Formula (IV), R⁸, at each occurrence, isindependently selected from the group consisting of C₁₋₆ alkyl andheterocycloalkyl; wherein the C₁₋₆ alkyl is independently optionallysubstituted with one or more OH; wherein the heterocycloalkylrepresented by R⁸ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofOH, F, Cl, Br and I.

In one embodiment of Formula (IV), R^(x) is selected from the groupconsisting of CN, F, Cl, Br and I. In another embodiment of Formula(IV), R^(x) is selected from the group consisting of F, Cl, Br and I. Inanother embodiment of Formula (IV), R^(x) is CN. In another embodimentof Formula (IV), R^(x) is F.

Still another embodiment pertains to compounds having Formula (VI),which include

-   2-[(4-fluorobenzyl)(propan-2-ylcarbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(3-methylbutyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-methylpropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-propoxyethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(tetrahydro    furan-2-ylmethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(1-methoxypropan-2-yl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-methoxyethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(2-ethoxyethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(1-methoxybutan-2-yl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(1,3-dioxolan-2-ylmethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl){[2-(propan-2-yloxy)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(1,4-dioxan-2-ylmethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(1,3-dimethoxypropan-2-yl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-fluorobenzyl)[(2-methoxybutyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(tetrahydrofuran-3-ylcarbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-fluorobenzyl)(tetrahydro-2H-pyran-3-ylcarbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[2-(propan-2-yloxy)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(2-methoxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[2-(2-hydroxyethoxy)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(propan-2-yloxy)propyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(3-hydroxy-2,2-dimethylpropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(2-hydroxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(1-hydroxypropan-2-yl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(3-hydroxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[(2S)-1-hydroxybut-3-en-2-yl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(4-hydroxybutyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{[(3-amino-3-oxopropyl)carbamoyl](4-cyanobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[3-(acetylamino)-2-methylpropyl]carbamoyl}(4-cyanobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(dimethylamino)-3-oxopropyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-{(4-cyanobenzyl)[(3-ethoxy-2-hydroxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(diethylamino)propyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[{[2-(acetylamino)ethyl]carbamoyl}(4-cyanobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[2-(diethylamino)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl)({2-[(2-methylpropanoyl)amino]ethyl}carbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[(2R)-1-hydroxybut-3-en-2-yl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   2-[(4-cyanobenzyl){[3-(3-hydroxyazetidin-1-yl)propyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   ethyl    N-[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]-beta-alaninate;-   ethyl    4-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoate;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoate;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-4-methylpentanoate;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2,2-dimethylpropanoate;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}cyclobutanecarboxylic    acid;-   ethyl    3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2-methylpropanoate;-   2-{(4-cyanobenzyl)[(3-methoxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoic    acid;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-4-methylpentanoic    acid;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2,2-dimethylpropanoic    acid;-   3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2-methylpropanoic    acid;-   N-[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]-beta-alanine;-   4-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoic    acid; and pharmaceutically acceptable salts thereof.    Pharmaceutical Compositions, Combination Therapies, Methods of    Treatment, and Administration

Another embodiment comprises pharmaceutical compositions comprising acompound having Formula (I) and an excipient.

Still another embodiment comprises methods of treating cancer in amammal comprising administering thereto a therapeutically acceptableamount of a compound having Formula (I).

Still another embodiment pertains to compositions for treating diseasesduring which NAMPT is expressed, said compositions comprising anexcipient and a therapeutically effective amount of the compound havingFormula (I).

Still another embodiment pertains to methods of treating disease in apatient during which NAMPT is expressed, said methods comprisingadministering to the patient a therapeutically effective amount of acompound having Formula (I).

Still another embodiment pertains to compositions for treatinginflammatory and tissue repair disorders; particularly rheumatoidarthritis, inflammatory bowel disease, asthma and COPD (chronicobstructive pulmonary disease), osteoarthritis, osteoporosis andfibrotic diseases; dermatosis, including psoriasis, atopic dermatitisand ultra-violet induced skin damage; autoimmune diseases includingsystemic lupus erythematosis, multiple sclerosis, psoriatic arthritis,ankylosing spondylitis, tissue and organ rejection, Alzheimer's disease,stroke, athersclerosis, restenosis, diabetes, glomerulonephritis,cancer, particularly wherein the cancer is selected from breast,prostate, lung, colon, cervix, ovary, skin, CNS, bladder, pancreas,leukemia, lymphoma or Hodgkin's disease, cachexia, inflammationassociated with infection and certain viral infections, includingAcquired Immune Deficiency Syndrome (AIDS), adult respiratory distresssyndrome, and ataxia telengiectasia, said compositions comprising anexcipient and a therapeutically effective amount of the compound havingFormula (I).

Still another embodiment pertains to methods of treating inflammatoryand tissue repair disorders; particularly rheumatoid arthritis,inflammatory bowel disease, asthma and COPD (chronic obstructivepulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases;dermatosis, including psoriasis, atopic dermatitis and ultra-violetinduced skin damage; autoimmune diseases including systemic lupuserythematosis, multiple sclerosis, psoriatic arthritis, ankylosingspondylitis, tissue and organ rejection, Alzheimer's disease, stroke,athersclerosis, restenosis, diabetes, glomerulonephritis, cancer,particularly wherein the cancer is selected from breast, prostate, lung,colon, cervix, ovary, skin, CNS, bladder, pancreas, leukemia, lymphomaor Hodgkin's disease, cachexia, inflammation associated with infectionand certain viral infections, including Acquired Immune DeficiencySyndrome (AIDS), adult respiratory distress syndrome, and ataxiatelengiectasia in a patient, said methods comprising administering tothe patient a therapeutically effective amount of a compound havingFormula (I).

Still another embodiment pertains to compositions for treating diseasesduring which NAMPT is expressed, said compositions comprising anexcipient and a therapeutically effective amount of the compound havingFormula (I) and a therapeutically effective amount of one additionaltherapeutic agent or more than one additional therapeutic agent.

Still another embodiment pertains to methods of treating disease in apatient during which NAMPT is expressed, said methods comprisingadministering to the patient a therapeutically effective amount of acompound having Formula (I) and a therapeutically effective amount ofone additional therapeutic agent or more than one additional therapeuticagent.

Still another embodiment pertains to compositions for treatinginflammatory and tissue repair disorders; particularly rheumatoidarthritis, inflammatory bowel disease, asthma and COPD (chronicobstructive pulmonary disease), osteoarthritis, osteoporosis andfibrotic diseases; dermatosis, including psoriasis, atopic dermatitisand ultra-violet induced skin damage; autoimmune diseases includingsystemic lupus erythematosis, multiple sclerosis, psoriatic arthritis,ankylosing spondylitis, tissue and organ rejection, Alzheimer's disease,stroke, athersclerosis, restenosis, diabetes, glomerulonephritis,cancer, particularly wherein the cancer is selected from breast,prostate, lung, colon, cervix, ovary, skin, CNS, bladder, pancreas,leukemia, lymphoma or Hodgkin's disease, cachexia, inflammationassociated with infection and certain viral infections, includingAcquired Immune Deficiency Syndrome (AIDS), adult respiratory distresssyndrome, and ataxia telengiectasia, said compositions comprising anexcipient and a therapeutically effective amount of the compound havingFormula (I) and a therapeutically effective amount of one additionaltherapeutic agent or more than one additional therapeutic agent.

Still another embodiment pertains to methods of treating inflammatoryand tissue repair disorders; particularly rheumatoid arthritis,inflammatory bowel disease, asthma and COPD (chronic obstructivepulmonary disease), osteoarthritis, osteoporosis and fibrotic diseases;dermatosis, including psoriasis, atopic dermatitis and ultra-violetinduced skin damage; autoimmune diseases including systemic lupuserythematosis, multiple sclerosis, psoriatic arthritis, ankylosingspondylitis, tissue and organ rejection, Alzheimer's disease, stroke,athersclerosis, restenosis, diabetes, glomerulonephritis, cancer,particularly wherein the cancer is selected from breast, prostate, lung,colon, cervix, ovary, skin, CNS, bladder, pancreas, leukemia, lymphomaor Hodgkin's disease, cachexia, inflammation associated with infectionand certain viral infections, including Acquired Immune DeficiencySyndrome (AIDS), adult respiratory distress syndrome, and ataxiatelengiectasia in a patient, said methods comprising administering tothe patient a therapeutically effective amount of the compound havingFormula (I) and a therapeutically effective amount of one additionaltherapeutic agent or more than one additional therapeutic agent.

Metabolites of compounds having Formula (I), produced by in vitro or invivo metabolic processes, may also have utility for treating diseasesassociated with NAMPT.

Certain precursor compounds which may be metabolized in vitro or in vivoto form compounds having Formula (I) may also have utility for treatingdiseases associated with NAMPT.

Compounds having Formula (I) may exist as acid addition salts, basicaddition salts or zwitterions. Salts of the compounds are preparedduring isolation or following purification of the compounds. Acidaddition salts of the compounds are those derived from the reaction ofthe compounds with an acid. For example, the acetate, adipate, alginate,bicarbonate, citrate, aspartate, benzoate, benzenesulfonate, bisulfate,butyrate, camphorate, camphorsulfonate, digluconate, formate, fumarate,glycerophosphate, glutamate, hemisulfate, heptanoate, hexanoate,hydrochloride, hydrobromide, hydroiodide, lactobionate, lactate,maleate, mesitylenesulfonate, methanesulfonate, naphthylenesulfonate,nicotinate, oxalate, pamoate, pectinate, persulfate, phosphate, picrate,propionate, succinate, tartrate, thiocyanate, trichloroacetic,trifluoroacetic, para-toluenesulfonate, and undecanoate salts of thecompounds are contemplated as being embraced by this invention. Basicaddition salts of the compounds are those derived from the reaction ofthe compounds with the hydroxide, carbonate or bicarbonate of cationssuch as lithium, sodium, potassium, calcium, and magnesium.

The compounds having Formula (I) may be administered, for example,bucally, ophthalmically, orally, osmotically, parenterally(intramuscularly, intraperitoneally intrasternally, intravenously,subcutaneously), rectally, topically, transdermally or vaginally.

Therapeutically effective amounts of compounds having Formula (I) dependon the recipient of the treatment, the disorder being treated and theseverity thereof, the composition containing the compound, the time ofadministration, the route of administration, the duration of treatment,the compound potency, its rate of clearance and whether or not anotherdrug is co-administered. The amount of a compound of this inventionhaving Formula (I) used to make a composition to be administered dailyto a patient in a single dose or in divided doses is from about 0.03 toabout 200 mg/kg body weight. Single dose compositions contain theseamounts or a combination of submultiples thereof.

Compounds having Formula (I) may be administered with or without anexcipient. Excipients include, for example, encapsulating materials oradditives such as absorption accelerators, antioxidants, binders,buffers, coating agents, coloring agents, diluents, disintegratingagents, emulsifiers, extenders, fillers, flavoring agents, humectants,lubricants, perfumes, preservatives, propellants, releasing agents,sterilizing agents, sweeteners, solubilizers, wetting agents andmixtures thereof.

Excipients for preparation of compositions comprising a compound havingFormula (I) to be administered orally in solid dosage form include, forexample, agar, alginic acid, aluminum hydroxide, benzyl alcohol, benzylbenzoate, 1,3-butylene glycol, carbomers, castor oil, cellulose,cellulose acetate, cocoa butter, corn starch, corn oil, cottonseed oil,cross-povidone, diglycerides, ethanol, ethyl cellulose, ethyl laureate,ethyl oleate, fatty acid esters, gelatin, germ oil, glucose, glycerol,groundnut oil, hydroxypropylmethyl cellulose, isopropanol, isotonicsaline, lactose, magnesium hydroxide, magnesium stearate, malt,mannitol, monoglycerides, olive oil, peanut oil, potassium phosphatesalts, potato starch, povidone, propylene glycol, Ringer's solution,safflower oil, sesame oil, sodium carboxymethyl cellulose, sodiumphosphate salts, sodium lauryl sulfate, sodium sorbitol, soybean oil,stearic acids, stearyl fumarate, sucrose, surfactants, talc, tragacanth,tetrahydrofurfuryl alcohol, triglycerides, water, and mixtures thereof.Excipients for preparation of compositions comprising a compound of thisinvention having Formula (I) to be administered ophthalmically or orallyin liquid dosage forms include, for example, 1,3-butylene glycol, castoroil, corn oil, cottonseed oil, ethanol, fatty acid esters of sorbitan,germ oil, groundnut oil, glycerol, isopropanol, olive oil, polyethyleneglycols, propylene glycol, sesame oil, water and mixtures thereof.Excipients for preparation of compositions comprising a compound of thisinvention having Formula (I) to be administered osmotically include, forexample, chlorofluorohydrocarbons, ethanol, water and mixtures thereof.Excipients for preparation of compositions comprising a compound of thisinvention having Formula (I) to be administered parenterally include,for example, 1,3-butanediol, castor oil, corn oil, cottonseed oil,dextrose, germ oil, groundnut oil, liposomes, oleic acid, olive oil,peanut oil, Ringer's solution, safflower oil, sesame oil, soybean oil,U.S.P. or isotonic sodium chloride solution, water and mixtures thereof.Excipients for preparation of compositions comprising a compound of thisinvention having Formula (I) to be administered rectally or vaginallyinclude, for example, cocoa butter, polyethylene glycol, wax andmixtures thereof.

Compounds having Formula (I) are expected to be useful when used withalkylating agents, angiogenesis inhibitors, antibodies, antimetabolites,antimitotics, antiproliferatives, antivirals, aurora kinase inhibitors,apoptosis promoters (for example, Bcl-xL, Bcl-w and Bfl-1) inhibitors,activators of death receptor pathway, Bcr-Abl kinase inhibitors, BiTE(Bi-Specific T cell Engager) antibodies, antibody drug conjugates,biologic response modifiers, cyclin-dependent kinase inhibitors, cellcycle inhibitors, cyclooxygenase-2 inhibitors, DVDs, leukemia viraloncogene homolog (ErbB2) receptor inhibitors, growth factor inhibitors,heat shock protein (HSP)-90 inhibitors, histone deacetylase (HDAC)inhibitors, hormonal therapies, immunologicals, inhibitors of inhibitorsof apoptosis proteins (IAPs), intercalating antibiotics, kinaseinhibitors, kinesin inhibitors, Jak2 inhibitors, mammalian target ofrapamycin inhibitors, microRNA's, mitogen-activated extracellularsignal-regulated kinase inhibitors, multivalent binding proteins,non-steroidal anti-inflammatory drugs (NSAIDs), poly ADP (adenosinediphosphate)-ribose polymerase (PARP) inhibitors, platinumchemotherapeutics, polo-like kinase (Plk) inhibitors, phosphoinositide-3kinase (PI3K) inhibitors, proteosome inhibitors, purine analogs,pyrimidine analogs, receptor tyrosine kinase inhibitors,retinoids/deltoids plant alkaloids, small inhibitory ribonucleic acids(siRNAs), topoisomerase inhibitors, ubiquitin ligase inhibitors, and thelike, and in combination with one or more of these agents.

BiTE antibodies are bi-specific antibodies that direct T-cells to attackcancer cells by simultaneously binding the two cells. The T-cell thenattacks the target cancer cell. Examples of BiTE antibodies includeadecatumumab (Micromet MT201), blinatumomab (Micromet MT103) and thelike. Without being limited by theory, one of the mechanisms by whichT-cells elicit apoptosis of the target cancer cell is by exocytosis ofcytolytic granule components, which include perforin and granzyme B.

SiRNAs are molecules having endogenous RNA bases or chemically modifiednucleotides. The modifications do not abolish cellular activity, butrather impart increased stability and/or increased cellular potency.Examples of chemical modifications include phosphorothioate groups,2′-deoxynucleotide, 2′-OCH₃-containing ribonucleotides,2′-F-ribonucleotides, 2′-methoxyethyl ribonucleotides, combinationsthereof and the like. The siRNA can have varying lengths (e.g., 10-200bps) and structures (e.g., hairpins, single/double strands, bulges,nicks/gaps, mismatches) and are processed in cells to provide activegene silencing. A double-stranded siRNA (dsRNA) can have the same numberof nucleotides on each strand (blunt ends) or asymmetric ends(overhangs). The overhang of 1-2 nucleotides can be present on the senseand/or the antisense strand, as well as present on the 5′- and/or the3′-ends of a given strand.

Multivalent binding proteins are binding proteins comprising two or moreantigen binding sites. Multivalent binding proteins are engineered tohave the three or more antigen binding sites and are generally notnaturally occurring antibodies. The term “multispecific binding protein”means a binding protein capable of binding two or more related orunrelated targets. Dual variable domain (DVD) binding proteins aretetravalent or multivalent binding proteins binding proteins comprisingtwo or more antigen binding sites. Such DVDs may be monospecific (i.e.,capable of binding one antigen) or multispecific (i.e., capable ofbinding two or more antigens). DVD binding proteins comprising two heavychain DVD polypeptides and two light chain DVD polypeptides are referredto as DVD Ig's. Each half of a DVD Ig comprises a heavy chain DVDpolypeptide, a light chain DVD polypeptide, and two antigen bindingsites. Each binding site comprises a heavy chain variable domain and alight chain variable domain with a total of 6 CDRs involved in antigenbinding per antigen binding site.

Alkylating agents include altretamine, AMD-473, AP-5280, apaziquone,bendamustine, brostallicin, busulfan, carboquone, carmustine (BCNU),chlorambucil, CLORETAZINE® (laromustine, VNP 40101M), cyclophosphamide,decarbazine, estramustine, fotemustine, glufosfamide, ifosfamide,KW-2170, lomustine (CCNU), mafosfamide, melphalan, mitobronitol,mitolactol, nimustine, nitrogen mustard N-oxide, ranimustine,temozolomide, thiotepa, TREANDA® (bendamustine), treosulfan,trofosfamide and the like.

Angiogenesis inhibitors include endothelial-specific receptor tyrosinekinase (Tie-2) inhibitors, epidermal growth factor receptor (EGFR)inhibitors, insulin growth factor-2 receptor (IGFR-2) inhibitors, matrixmetalloproteinase-2 (MMP-2) inhibitors, matrix metalloproteinase-9(MMP-9) inhibitors, platelet-derived growth factor receptor (PDGFR)inhibitors, thrombospondin analogs, vascular endothelial growth factorreceptor tyrosine kinase (VEGFR) inhibitors and the like.

Antimetabolites include ALIMTA® (pemetrexed disodium, LY231514, MTA),5-azacitidine, XELODA® (capecitabine), carmofur, LEUSTAT® (cladribine),clofarabine, cytarabine, cytarabine ocfosfate, cytosine arabinoside,decitabine, deferoxamine, doxifluridine, eflornithine, EICAR(5-ethynyl-1-β-D-ribofuranosylimidazole-4-carboxamide), enocitabine,ethnylcytidine, fludarabine, 5-fluorouracil alone or in combination withleucovorin, GEMZAR® (gemcitabine), hydroxyurea, ALKERAN® (melphalan),mercaptopurine, 6-mercaptopurine riboside, methotrexate, mycophenolicacid, nelarabine, nolatrexed, ocfosfate, pelitrexol, pentostatin,raltitrexed, Ribavirin, triapine, trimetrexate, S-1, tiazofurin,tegafur, TS-1, vidarabine, UFT and the like.

Antivirals include ritonavir, hydroxychloroquine and the like.

Aurora kinase inhibitors include ABT-348, AZD-1152, MLN-8054, VX-680,Aurora A-specific kinase inhibitors, Aurora B-specific kinase inhibitorsand pan-Aurora kinase inhibitors and the like.

Bcl-2 protein inhibitors include AT-101 ((−)gossypol), GENASENSE® (G3139or oblimersen (Bcl-2-targeting antisense oligonucleotide)), IPI-194,IPI-565,N-(4-(4-((4′-chloro(1,1′-biphenyl)-2-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(dimethylamino)-1-((phenylsulfanyl)methyl)propyl)amino)-3-nitrobenzenesulfonamide)(ABT-737),N-(4-(4-((2-(4-chlorophenyl)-5,5-dimethyl-1-cyclohex-1-en-1-yl)methyl)piperazin-1-yl)benzoyl)-4-(((1R)-3-(morpholin-4-yl)-1-((phenylsulfanyl)methyl)propyl)amino)-3-((trifluoromethyl)sulfonyl)benzenesulfonamide(ABT-263), GX-070 (obatoclax) and the like.

Bcr-Abl kinase inhibitors include DASATINIB® (BMS-354825), GLEEVEC®(imatinib) and the like.

CDK inhibitors include AZD-5438, BMI-1040, BMS-032, BMS-387, CVT-2584,flavopyridol, GPC-286199, MCS-5A, PD0332991, PHA-690509, seliciclib(CYC-202, R-roscovitine), ZK-304709 and the like.

COX-2 inhibitors include ABT-963, ARCOXIA® (etoricoxib), BEXTRA®(valdecoxib), BMS347070, CELEBREX® (celecoxib), COX-189 (lumiracoxib),CT-3, DERAMAXX® (deracoxib), JTE-522,4-methyl-2-(3,4-dimethylphenyl)-1-(4-sulfamoylphenyl-1H-pyrrole), MK-663(etoricoxib), NS-398, parecoxib, RS-57067, SC-58125, SD-8381, SVT-2016,S-2474, T-614, VIOXX® (rofecoxib) and the like.

EGFR inhibitors include ABX-EGF, anti-EGFR immunoliposomes, EGF-vaccine,EMD-7200, ERBITUX® (cetuximab), HR3, IgA antibodies, IRESSA®(gefitinib), TARCEVA® (erlotinib or OSI-774), TP-38, EGFR fusionprotein, TYKERB® (lapatinib) and the like.

ErbB2 receptor inhibitors include CP-724-714, CI-1033 (canertinib),HERCEPTIN® (trastuzumab), TYKERB® (lapatinib), OMNITARG® (2C4,petuzumab), TAK-165, GW-572016 (ionafarnib), GW-282974, EKB-569, PI-166,dHER2 (HER2 vaccine), APC-8024 (HER-2 vaccine), anti-HER/2neu bispecificantibody, B7.her2IgG3, AS HER2 trifunctional bispecific antibodies, mABAR-209, mAB 2B-1 and the like.

Histone deacetylase inhibitors include depsipeptide, LAQ-824, MS-275,trapoxin, suberoylanilide hydroxamic acid (SAHA), TSA, valproic acid andthe like.

HSP-90 inhibitors include 17-AAG-nab, 17-AAG, CNF-101, CNF-1010,CNF-2024, 17-DMAG, geldanamycin, IPI-504, KOS-953, MYCOGRAB® (humanrecombinant antibody to HSP-90), NCS-683664, PU24FC1, PU-3, radicicol,SNX-2112, STA-9090 VER49009 and the like.

Inhibitors of inhibitors of apoptosis proteins include HGS1029,GDC-0145, GDC-0152, LCL-161, LBW-242 and the like.

Antibody drug conjugates include anti-CD22-MC-MMAF, anti-CD22-MC-MMAE,anti-CD22-MCC-DM1, CR-011-vcMMAE, PSMA-ADC, MEDI-547, SGN-19Am SGN-35,SGN-75 and the like

Activators of death receptor pathway include TRAIL, antibodies or otheragents that target TRAIL or death receptors (e.g., DR4 and DR5) such asApomab, conatumumab, ETR2-ST01, GDC0145 (lexatumumab), HGS-1029,LBY-135, PRO-1762 and trastuzumab.

Kinesin inhibitors include Eg5 inhibitors such as AZD4877, ARRY-520;CENPE inhibitors such as GSK923295A and the like.

JAK-2 inhibitors include CEP-701 (lesaurtinib), XL019 and INCB018424 andthe like.

MEK inhibitors include ARRY-142886, ARRY-438162 PD-325901, PD-98059 andthe like.

mTOR inhibitors include AP-23573, CCI-779, everolimus, RAD-001,rapamycin, temsirolimus, ATP-competitive TORC1/TORC2 inhibitors,including PI-103, PP242, PP30, Torin 1 and the like.

Non-steroidal anti-inflammatory drugs include AMIGESIC® (salsalate),DOLOBID® (diflunisal), MOTRIN® (ibuprofen), ORUDIS® (ketoprofen),RELAFEN® (nabumetone), FELDENE® (piroxicam), ibuprofen cream, ALEVE®(naproxen) and NAPROSYN® (naproxen), VOLTAREN® (diclofenac), INDOCIN®(indomethacin), CLINORIL® (sulindac), TOLECTIN® (tolmetin), LODINE®(etodolac), TORADOL® (ketorolac), DAYPRO® (oxaprozin) and the like.

PDGFR inhibitors include C-451, CP-673, CP-868596 and the like.

Platinum chemotherapeutics include cisplatin, ELOXATIN® (oxaliplatin)eptaplatin, lobaplatin, nedaplatin, PARAPLATIN® (carboplatin),satraplatin, picoplatin and the like.

Polo-like kinase inhibitors include BI-2536 and the like.

Phosphoinositide-3 kinase (PI3K) inhibitors include wortmannin,LY294002, XL-147, CAL-120, ONC-21, AEZS-127, ETP-45658, PX-866,GDC-0941, BGT226, BEZ235, XL765 and the like.

Thrombospondin analogs include ABT-510, ABT-567, ABT-898, TSP-1 and thelike.

VEGFR inhibitors include AVASTIN® (bevacizumab), ABT-869, AEE-788,ANGIOZYME™ (a ribozyme that inhibits angiogenesis (RibozymePharmaceuticals (Boulder, Colo.) and Chiron, (Emeryville, Calif.)),axitinib (AG-13736), AZD-2171, CP-547,632, IM-862, MACUGEN (pegaptamib),NEXAVAR® (sorafenib, BAY43-9006), pazopanib (GW-786034), vatalanib(PTK-787, ZK-222584), SUTENT® (sunitinib, SU-11248), VEGF trap, ZACTIMA™(vandetanib, ZD-6474) and the like.

Antibiotics include intercalating antibiotics aclarubicin, actinomycinD, amrubicin, annamycin, adriamycin, BLENOXANE® (bleomycin),daunorubicin, CAELYX® or MYOCET® (liposomal doxorubicin), elsamitrucin,epirbucin, glarbuicin, ZAVEDOS® (idarubicin), mitomycin C, nemorubicin,neocarzinostatin, peplomycin, pirarubicin, rebeccamycin, stimalamer,streptozocin, VALSTAR® (valrubicin), zinostatin and the like.

Topoisomerase inhibitors include aclarubicin, 9-aminocamptothecin,amonafide, amsacrine, becatecarin, belotecan, BN-80915, CAMPTOSAR®(irinotecan hydrochloride), camptothecin, CARDIOXANE® (dexrazoxine),diflomotecan, edotecarin, ELLENCE® or PHARMORUBICIN® (epirubicin),etoposide, exatecan, 10-hydroxycamptothecin, gimatecan, lurtotecan,mitoxantrone, orathecin, pirarbucin, pixantrone, rubitecan, sobuzoxane,SN-38, tafluposide, topotecan and the like.

Antibodies include AVASTIN® (bevacizumab), CD40-specific antibodies,chTNT-1/B, denosumab, ERBITUX® (cetuximab), HUMAX-CD4® (zanolimumab),IGF1R-specific antibodies, lintuzumab, PANOREX® (edrecolomab), RENCAREX®(WX G250), RITUXAN® (rituximab), ticilimumab, trastuzimab, CD20antibodies types I and II and the like.

Hormonal therapies include ARIMIDEX® (anastrozole), AROMASIN®(exemestane), arzoxifene, CASODEX® (bicalutamide), CETROTIDE®(cetrorelix), degarelix, deslorelin, DESOPAN® (trilostane),dexamethasone, DROGENIL® (flutamide), EVISTA® (raloxifene), AFEMA™(fadrozole), FARESTON® (toremifene), FASLODEX® (fulvestrant), FEMARA®(letrozole), formestane, glucocorticoids, HECTOROL® (doxercalciferol),RENAGEL® (sevelamer carbonate), lasofoxifene, leuprolide acetate,MEGACE® (megesterol), MIFEPREX® (mifepristone), NILANDRON™ (nilutamide),NOLVADEX® (tamoxifen citrate), PLENAXIS™ (abarelix), prednisone,PROPECIA® (finasteride), rilostane, SUPREFACT® (buserelin), TRELSTAR®(luteinizing hormone releasing hormone (LHRH)), VANTAS® (Histrelinimplant), VETORYL® (trilostane or modrastane), ZOLADEX® (fosrelin,goserelin) and the like.

Deltoids and retinoids include seocalcitol (EB1089, CB1093),lexacalcitrol (KH1060), fenretinide, PANRETIN® (aliretinoin), ATRAGEN®(liposomal tretinoin), TARGRETIN® (bexarotene), LGD-1550 and the like.

PARP inhibitors include ABT-888 (veliparib), olaparib, KU-59436,AZD-2281, AG-014699, BSI-201, BGP-15, INO-1001, ONO-2231 and the like.

Plant alkaloids include, but are not limited to, vincristine,vinblastine, vindesine, vinorelbine and the like.

Proteasome inhibitors include VELCADE® (bortezomib), MG132, NPI-0052,PR-171 and the like.

Examples of immunologicals include interferons and otherimmune-enhancing agents. Interferons include interferon alpha,interferon alpha-2a, interferon alpha-2b, interferon beta, interferongamma-1a, ACTIMMUNE® (interferon gamma-1b) or interferon gamma-n1,combinations thereof and the like. Other agents include ALFAFERONE®,(IFN-α), BAM-002 (oxidized glutathione), BEROMUN® (tasonermin), BEXXAR®(tositumomab), CAMPATH® (alemtuzumab), CTLA4 (cytotoxic lymphocyteantigen 4), decarbazine, denileukin, epratuzumab, GRANOCYTE®(lenograstim), lentinan, leukocyte alpha interferon, imiquimod, MDX-010(anti-CTLA-4), melanoma vaccine, mitumomab, molgramostim, MYLOTARG™(gemtuzumab ozogamicin), NEUPOGEN® (filgrastim), OncoVAC-CL, OVAREX®(oregovomab), pemtumomab (Y-muHMFG1), PROVENGE® (sipuleucel-T),sargaramostim, sizofilan, teceleukin, THERACYS® (BacillusCalmette-Guerin), ubenimex, VIRULIZIN® (immunotherapeutic, LorusPharmaceuticals), Z-100 (Specific Substance of Maruyama (SSM)), WF-10(Tetrachlorodecaoxide (TCDO)), PROLEUKIN® (aldesleukin), ZADAXIN®(thymalfasin), ZENAPAX® (daclizumab), ZEVALIN® (90Y-Ibritumomabtiuxetan) and the like.

Biological response modifiers are agents that modify defense mechanismsof living organisms or biological responses, such as survival, growth ordifferentiation of tissue cells to direct them to have anti-tumoractivity and include krestin, lentinan, sizofuran, picibanil PF-3512676(CpG-8954), ubenimex and the like.

Pyrimidine analogs include cytarabine (ara C or Arabinoside C), cytosinearabinoside, doxifluridine, FLUDARA® (fludarabine), 5-FU(5-fluorouracil), floxuridine, GEMZAR® (gemcitabine), TOMUDEX®(ratitrexed), TROXATYL™ (triacetyluridine troxacitabine) and the like.

Purine analogs include LANVIS® (thioguanine) and PURI-NETHOL®(mercaptopurine).

Antimitotic agents include batabulin, epothilone D (KOS-862),N-(2-((4-hydroxyphenyl)amino)pyridin-3-yl)-4-methoxybenzenesulfonamide,ixabepilone (BMS 247550), paclitaxel, TAXOTERE® (docetaxel), PNU100940(109881), patupilone, XRP-9881 (larotaxel), vinflunine, ZK-EPO(synthetic epothilone) and the like.

Ubiquitin ligase inhibitors include MDM2 inhibitors, such as nutlins,NEDD8 inhibitors such as MLN4924 and the like.

Compounds of this invention can also be used as radiosensitizers thatenhance the efficacy of radiotherapy. Examples of radiotherapy includeexternal beam radiotherapy, teletherapy, brachytherapy and sealed,unsealed source radiotherapy and the like.

Additionally, compounds having Formula (I) may be combined with otherchemotherapeutic agents such as ABRAXANE™ (ABI-007), ABT-100 (farnesyltransferase inhibitor), ADVEXIN® (Ad5CMV-p53 vaccine), ALTOCOR® orMEVACOR® (lovastatin), AMPLIGEN® (poly I:poly C12U, a synthetic RNA),APTOSYN® (exisulind), AREDIA® (pamidronic acid), arglabin,L-asparaginase, atamestane (1-methyl-3,17-dione-androsta-1,4-diene),AVAGE® (tazarotene), AVE-8062 (combreastatin derivative) BEC2(mitumomab), cachectin or cachexin (tumor necrosis factor), canvaxin(vaccine), CEAVAC® (cancer vaccine), CELEUK® (celmoleukin), CEPLENE®(histamine dihydrochloride), CERVARIX® (human papillomavirus vaccine),CHOP® (C: CYTOXAN® (cyclophosphamide); H: ADRIAMYCIN®(hydroxydoxorubicin); O: Vincristine (ONCOVIN®); P: prednisone), CYPAT™(cyproterone acetate), combrestatin A4P, DAB(389)EGF (catalytic andtranslocation domains of diphtheria toxin fused via a His-Ala linker tohuman epidermal growth factor) or TransMID-107R™ (diphtheria toxins),dacarbazine, dactinomycin, 5,6-dimethylxanthenone-4-acetic acid (DMXAA),eniluracil, EVIZON™ (squalamine lactate), DIMERICINE® (T4N5 liposomelotion), discodermolide, DX-8951f (exatecan mesylate), enzastaurin,EPO906 (epithilone B), GARDASIL® (quadrivalent human papillomavirus(Types 6, 11, 16, 18) recombinant vaccine), GASTRIMMUNE®, GENASENSE®,GMK (ganglioside conjugate vaccine), GVAX® (prostate cancer vaccine),halofuginone, histerelin, hydroxycarbamide, ibandronic acid, IGN-101,IL-13-PE38, IL-13-PE38QQR (cintredekin besudotox), IL-13-pseudomonasexotoxin, interferon-α, interferon-γ, JUNOVAN™ or MEPACT™ (mifamurtide),lonafarnib, 5,10-methylenetetrahydrofolate, miltefosine(hexadecylphosphocholine), NEOVASTAT® (AE-941), NEUTREXIN® (trimetrexateglucuronate), NIPENT® (pentostatin), ONCONASE® (a ribonuclease enzyme),ONCOPHAGE® (melanoma vaccine treatment), ONCOVAX® (IL-2 Vaccine),ORATHECIN™ (rubitecan), OSIDEM® (antibody-based cell drug), OVAREX® MAb(murine monoclonal antibody), paclitaxel, PANDIMEX™ (aglycone saponinsfrom ginseng comprising 20(S)protopanaxadiol (aPPD) and20(S)protopanaxatriol (aPPT)), panitumumab, PANVAC®-VF (investigationalcancer vaccine), pegaspargase, PEG Interferon A, phenoxodiol,procarbazine, rebimastat, REMOVAB® (catumaxomab), REVLIMID®(lenalidomide), RSR13 (efaproxiral), SOMATULINE® LA (lanreotide),SORIATANE® (acitretin), staurosporine (Streptomyces staurospores),talabostat (PT100), TARGRETIN® (bexarotene), TAXOPREXIN®(DHA-paclitaxel), TELCYTA® (canfosfamide, TLK286), temilifene, TEMODAR®(temozolomide), tesmilifene, thalidomide, THERATOPE® (STn-KLH), thymitaq(2-amino-3,4-dihydro-6-methyl-4-oxo-5-(4-pyridylthio)quinazolinedihydrochloride), TNFERADE™ (adenovector: DNA carrier containing thegene for tumor necrosis factor-α), TRACLEER® or ZAVESCA® (bosentan),tretinoin (Retin-A), tetrandrine, TRISENOX® (arsenic trioxide),VIRULIZIN®, ukrain (derivative of alkaloids from the greater celandineplant), vitaxin (anti-alphavbeta3 antibody), XCYTRIN® (motexafingadolinium), XINLAY™ (atrasentan), XYOTAX™ (paclitaxel poliglumex),YONDELIS® (trabectedin), ZD-6126, ZINECARD® (dexrazoxane), ZOMETA®(zolendronic acid), zorubicin and the like.

Data

Determination of the utility of compounds having Formula (I) as bindersto and inhibitors of NAMPT was performed using Time-ResolvedFluorescence Resonance Energy Transfer (TR-FRET) binding assays.

Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) BindingAssay of NAMPT

Test compounds were serially diluted (typically 11 half log dilutions)in neat DMSO to 50× final concentrations prior to dilution with assaybuffer (50 mM HEPES (NaOH), pH 7.5, 100 mM NaCl, 10 mM MgCl₂, 1 mM DTT,1% Glycerol) to 3× and 6% DMSO. Six μL were transferred to 384-welllow-volume plates (Owens Corning #3673). To this, 12 μL of a 1.5×solution containing enzyme, probe and antibody were added. Finalconcentrations in the 18 μL reactions were 1× assay buffer, 2% DMSO, 6.8nM NAMPT (human, recombinant, C-terminally His-tagged), 200 nM probe (apotent nicotinamide-competitive inhibitor conjugated to Oregon Green488) and 1 nM Tb-anti-His antibody (Invitrogen #PV5895). Reactions wereequilibrated at room temperature for 3 hours prior to reading on anEnvision multi-label plate reader (Perkin Elmer; Ex=337 nm, Em=520 and495 nm). Time-resolved FRET ratios (Em₅₂₀/Em₄₉₅) were normalized tocontrols, plotted as a function of compound concentration and fit withthe four-parameter logistic equation to determine IC50s.

Time-Resolved Fluorescence Resonance Energy Transfer (TR-FRET) BindingAssay of NAMPT with PRPP

Compound handling and data processing were identical to the assay in theabsence of substrates (above). Final concentrations were 1× assaybuffer, 2% DMSO, 2 nM NAMPT, 2 nM probe, 1 nM Tb-anti-His antibody(Invitrogen #PV5895), 200 μM PRPP and 2.5 mM ATP. Reactions wereequilibrated for 16 hours prior to measurement to allow for potentialenzymatic modification of test compounds.

Table 1 shows the utility of compounds having Formula I to functionallyinhibit NAMPT.

TABLE 1 TR-FRET Binding - TR-FRET Binding - Example IC50 (μM) IC50 (withPRPP) (μM) 1 0.0638 nd 2 7.56 0.00429 3 12.5 0.0715 4 1.22 0.000548 50.72 0.000461 6 nd nd 7 1.61 0.486 8 3.16 0.29 9 12.5 0.641 10 0.2810.0196 11 0.476 0.00047 12 0.303 0.000241 13 1.75 0.000403 14 12.5 0.33815 3.82 0.0921 16 4.72 0.217 17 12.5 1.22 18 4.82 0.814 19 12.5 12.5 2012.5 12.5 21 0.996 0.505 22 0.384 0.0602 23 nd nd 24 4.14 0.000682 251.63 0.0014 26 12.5 0.00121 27 >10 0.000632 28 7.02 0.000833 29 >100.00216 30 >10 0.00229 31 3.6 0.000893 32 >10 0.00133 33 8.95 0.00122 347.57 0.000502 35 >10 0.00318 36 2.42 0.000725 37 4.81 0.000531 38 2.690.00135 39 2.39 0.000938 40 2.2 0.00199 41 8.5 0.0297 42 >10 0.0246 438.11 0.000709 44 >10 0.00777 45 0.611 0.000206 46 9.52 0.0022 47 nd nd48 0.807 0.000701 49 1.69 0.00107 50 1.18 0.00252 51 >10 0.00494 52 1.010.000881 53 2.53 0.32 54 2.11 0.0056 55 >10 3.18 56 6.07 0.000719 57 >101.16 58 1.72 0.807 59 >10 0.266 60 >10 0.00497 61 1.9 0.00178 62 0.810.00108 63 2.25 0.000693 64 1.85 0.00297 65 >10 0.00537 66 >10 0.0024267 >10 0.00353 68 >10 0.00468 69 >10 0.00398 70 >10 0.00508 71 0.5330.0007 72 >10 0.00399 73 >10 0.00704 74 nd nd 75 nd nd 76 nd nd 770.0956 0.000774 78 2.9 0.000969 79 6.58 0.00277 80 8.02 0.00137 81 5.280.00178 82 7.54 0.00172 83 2.89 0.000998 84 3.2 0.00172 85 nd nd 86 >100.00266 87 2.26 0.00126 88 >10 0.000602 89 5.83 0.00198 90 >10 0.0022591 8.69 0.000543 92 >10 0.000868 93 >10 0.0166 94 2.87 0.00122 95 3.890.0151 96 4.19 0.00335 97 >10 0.00589 98 1.5 0.00147 99 3.56 0.0015 100nd nd 101 5.62 0.00284 102 0.306 0.00216 103 0.709 0.00306 104 0.4450.00131 105 nd nd 106 1.93 0.0018 107 0.814 0.00224 108 1.45 0.00161109 >10 0.00374 110 >10 0.0232 111 >10 0.00587 112 3.68 0.00208 113 4.990.00676 114 1.99 0.00231 115 1.42 0.0036 116 nd nd 117 1.25 0.00302 118nd nd 119 4.57 0.00189 120 3.78 0.00229 121 >10 0.00925 122 >10 0.00431123 3.82 0.000631 124 3.52 0.000624 125 >10 0.000712 126 4.18 0.0013 1273.18 0.000533 128 >10 0.000727 129 >10 0.00116 130 >10 0.00111 131 4.780.000743 132 4.85 0.00102 133 0.0589 0.000527 134 0.2 0.000617 1350.0937 0.000169 136 0.0244 0.000174 137 0.0402 0.000236 138 0.05550.000541 139 0.0561 0.000251 140 >10 0.0223 141 >10 0.0231 142 6.040.0169 143 >10 0.0137 144 >10 0.0332 145 >10 0.107 146 >10 0.098 147 >100.0719 148 >10 0.0606 149 >10 0.0942 150 0.252 0.00021 151 0.2190.000412 152 0.768 0.000232 153 1.43 0.000286 154 0.23 0.000518 1550.669 0.000254 156 nd nd 157 nd nd 158 nd nd 159 8.23 0.291 160 >100.195 161 >10 0.215 162 3.33 0.187 163 6.8 0.171 164 >10 0.583 165 0.340.0991 166 >10 0.63 167 nd nd 168 >10 1.39 169 8.45 0.266 170 nd nd 1718.79 0.0321 172 >10 0.153 173 0.707 0.00233 174 0.334 0.000714 175 1.150.0006 176 7.36 0.000365 177 4.62 0.000653 178 6.97 0.000813 179 9.80.000492 180 7.71 0.000333 181 >10 0.000556 182 2.59 0.000264 183 2.940.000281 184 0.763 0.000285 185 0.633 0.000476 186 1.1 0.00123 187 3.210.000216 188 0.356 0.000195 189 4.7 0.000586 190 2.61 0.000606 191 >100.000265 192 >10 0.000262 193 6.06 0.000755 194 7.25 0.00112 195 >100.000338 196 7.01 0.000538 197 9.21 0.000251 198 2.61 0.000633 199 >100.000493 200 >10 0.000747 201 >10 0.000457 202 4.99 0.000405 203 >100.0136 204 3.73 0.00146 205 0.739 0.000177 206 5.63 0.000633 207 3.860.000331 208 2.89 0.00025 209 6.7 0.000245 210 2.74 0.000192 211 nd nd212 5.71 0.00103 213 9.86 0.000411 nd = no data

Compounds which inhibit NAMPT are useful for treating diseases in whichactivation of NF-KB is implicated. Such methods are useful in thetreatment of a variety of diseases including inflammatory and tissuerepair disorders; particularly rheumatoid arthritis, inflammatory boweldisease, asthma and COPD (chronic obstructive pulmonary disease),osteoarthritis, osteoporosis and fibrotic diseases; dermatosis,including psoriasis, atopic dermatitis and ultra-violet induced skindamage; autoimmune diseases including systemic lupus erythematosis,multiple sclerosis, psoriatic arthritis, ankylosing spondylitis, tissueand organ rejection, Alzheimer's disease, stroke, athersclerosis,restenosis, diabetes, glomerulonephritis, cancer, particularly whereinthe cancer is selected from breast, prostate, lung, colon, cervix,ovary, skin, CNS, bladder, pancreas, leukaemia, lymphoma or Hodgkin'sdisease, cachexia, inflammation associated with infection and certainviral infections, including Acquired Immune Deficiency Syndrome (AIDS),adult respiratory distress syndrome, and ataxia telengiectasia.

Involvement of NAMPT in the treatment of cancer is described in WO97/48696. Involvement of NAMPT in immuno-suppression is described in WO97/48397. Involvement of NAMPT for the treatment of diseases involvingangiogenesis is described in WO 2003/80054. Involvement of NAMPT for thetreatment of rheumatoid arthritis and septic shock is described in WO2008/025857. Involvement of NAMPT for the prophylaxis and treatment ofischaemia is described in WO 2009/109610.

Cancers include, but are not limited to, hematologic and solid tumortypes such as acoustic neuroma, acute leukemia, acute lymphoblasticleukemia, acute myelogenous leukemia (monocytic, myeloblastic,adenocarcinoma, angiosarcoma, astrocytoma, myelomonocytic andpromyelocytic), acute t-cell leukemia, basal cell carcinoma, bile ductcarcinoma, bladder cancer, brain cancer, breast cancer (includingestrogen-receptor positive breast cancer), bronchogenic carcinoma,Burkitt's lymphoma, cervical cancer, chondrosarcoma, chordoma,choriocarcinoma, chronic leukemia, chronic lymphocytic leukemia, chronicmyelocytic (granulocytic) leukemia, chronic myelogenous leukemia, coloncancer, colorectal cancer, craniopharyngioma, cystadenocarcinoma,dysproliferative changes (dysplasias and metaplasias), embryonalcarcinoma, endometrial cancer, endotheliosarcoma, ependymoma, epithelialcarcinoma, erythroleukemia, esophageal cancer, estrogen-receptorpositive breast cancer, essential thrombocythemia, Ewing's tumor,fibrosarcoma, gastric carcinoma, germ cell testicular cancer,gestational trophoblastic disease, glioblastoma, head and neck cancer,heavy chain disease, hemangioblastoma, hepatoma, hepatocellular cancer,hormone insensitive prostate cancer, leiomyosarcoma, liposarcoma, lungcancer (including small cell lung cancer and non-small cell lungcancer), lymphangioendothelio-sarcoma, lymphangiosarcoma, lymphoblasticleukemia, lymphoma (lymphoma, including diffuse large B-cell lymphoma,follicular lymphoma, Hodgkin's lymphoma and non-Hodgkin's lymphoma),malignancies and hyperproliferative disorders of the bladder, breast,colon, lung, ovaries, pancreas, prostate, skin and uterus, lymphoidmalignancies of T-cell or B-cell origin, leukemia, medullary carcinoma,medulloblastoma, melanoma, meningioma, mesothelioma, multiple myeloma,myelogenous leukemia, myeloma, myxosarcoma, neuroblastoma,oligodendroglioma, oral cancer, osteogenic sarcoma, ovarian cancer,pancreatic cancer, papillary adenocarcinomas, papillary carcinoma,peripheral T-cell lymphoma, pinealoma, polycythemia vera, prostatecancer (including hormone-insensitive (refractory) prostate cancer),rectal cancer, renal cell carcinoma, retinoblastoma, rhabdomyosarcoma,sarcoma, sebaceous gland carcinoma, seminoma, skin cancer, small celllung carcinoma, solid tumors (carcinomas and sarcomas), stomach cancer,squamous cell carcinoma, synovioma, sweat gland carcinoma, testicularcancer (including germ cell testicular cancer), thyroid cancer,Waldenström's macroglobulinemia, testicular tumors, uterine cancer,Wilms' tumor and the like.

Schemes and Experimentals

The following abbreviations have the meanings indicated. ADDP means1,1′-(azodicarbonyl)dipiperidine; AD-mix-β means a mixture of(DHQD)₂PHAL, K₃Fe(CN)₆, K₂CO₃, and K₂SO₄; 9-BBN means9-borabicyclo(3.3.1)nonane; Boc means tert-butoxycarbonyl; (DHQD)₂PHALmeans hydroquinidine 1,4-phthalazinediyl diethyl ether; DBU means1,8-diazabicyclo[5.4.0]undec-7-ene; DIBAL means diisobutylaluminumhydride; DIEA means diisopropylethylamine; DMAP meansN,N-dimethylaminopyridine; DMF means N,N-dimethylformamide; dmpe means1,2-bis(dimethylphosphino)ethane; DMSO means dimethylsulfoxide; dppbmeans 1,4-bis(diphenylphosphino)-butane; dppe means1,2-bis(diphenylphosphino)ethane; dppf means1,1′-bis(diphenylphosphino)ferrocene; dppm means1,1-bis(diphenylphosphino)methane; EDAC.HCl means1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride; Fmoc meansfluorenylmethoxycarbonyl; HATU meansO-(7-azabenzotriazol-1-yl)-N,N′N′N′-tetramethyluroniumhexafluorophosphate; HMPA means hexamethylphosphoramide; IPA meansisopropyl alcohol; MP-BH₃ means macroporous triethylammoniummethylpolystyrene cyanoborohydride; TEA means triethylamine; TFA meanstrifluoroacetic acid; THF means tetrahydrofuran; NCS meansN-chlorosuccinimide; NMM means N-methylmorpholine; NMP meansN-methylpyrrolidine; PPh₃ means triphenylphosphine.

The following schemes are presented to provide what is believed to bethe most useful and readily understood description of procedures andconceptual aspects of this invention. Compounds of this invention may bemade by synthetic chemical processes, examples of which are shownherein. It is meant to be understood that the order of the steps in theprocesses may be varied, that reagents, solvents and reaction conditionsmay be substituted for those specifically mentioned, and that vulnerablemoieties may be protected and deprotected, as necessary.

Schemes

As shown in Scheme 1,2-bromothiazole-5-carboxylic acid can be coupledwith a suitable amine of formula (1), wherein R³, R⁴, and R⁵ are asdescribed herein, under reaction conditions known to those skilled inthe art and readily available in the literature, to provide compounds offormula (2). Compounds of formula (2) can be reacted with suitableamines of formula (3), wherein R⁶ is as described herein, to providecompounds of formula (4). The reaction is typically performed at anelevated temperature in a solvent such as but not limited toacetonitrile. Compounds of formula (6), which are representative ofcompounds of Formula (I), can be prepared by reacting compounds offormula (4) with a suitable compound of formula (5), wherein R⁶ asdescribed herein. The reaction is typically performed in a suitablesolvent such as but not limited to dichloromethane at ambienttemperature in the presence of a base such as but not limited topyridine.

Compounds of formula (4), which can be prepared as described in Scheme1, can be reacted with bis(2,5-dioxopyrrolidin-1-yl)carbonate at anelevated temperature in the presence of a base such as but not limitedto pyridine, followed by the addition of a base such as but not limitedto N,N-diisopropylethylamine, and an amine of formula (3) to providecompounds of formula (6) which are representative of the compounds ofFormula (I).

As shown in Scheme 3, compounds of formula (4), which can be prepared asdescribed in Scheme 1, can be reacted with a suitable alkyl halide offormula (7), wherein X is an appropriate halide and R⁶ is as describedherein, to provide compounds of formula (8), which are representative ofthe compounds of Formula (I). The reaction is typically performed at anelevated temperature in a suitable solvent such as but not limited toacetonitrile, and may involve the use of microwave heating.

Compounds of formula (4), which can be prepared as described in Scheme1, can be reacted with compounds of formula (9), wherein R⁶ is asdescribed herein, in the presence of a base such as but not limited toN,N-diisopropylethylamine, to provide compounds of formula (10), whichare representative of the compounds of Formula (I). The reaction istypically performed at an elevated temperature in a suitable solventsuch as but not limited to dimethylsulfoxide, methanol, or mixturesthereof.

As shown in Scheme 5, chloroacetyl bromide can be reacted with compoundsof formula (4), which can be prepared as described in Scheme 5, in thepresence of a base such as but not limited to pyridine, at a reducedtemperature followed by reaction with a suitable amine of formula (11),wherein each R⁸ is as described herein, at an elevated temperature, toprovide compounds of formula (12). The reaction is typically performedin a solvent such as but not limited to dichloromethane.

As shown in Scheme 6, compounds of formula (2), which can be prepared asdescribed in Scheme 1, can be coupled with a suitable amine of formula(13), wherein R¹ and R² taken together with the N to which they areattached form a heterocycloalkyl or heterocycloalkenyl ring, to providecompounds of formula (14). The reaction is typically performed at anelevated temperature in the presence of potassium phosphate, a catalystsuch as but not limited to tris(dibenzylideneacetone)dipalladium(0), anda ligand such as but not limited to4,5-bis(diphenylphosphino)-9,9-dimethylxanthene (XantPhos). The reactionis typically performed in a suitable solvent such as but not limited todioxane.

EXAMPLES

The following examples are presented to provide what is believed to bethe most useful and readily understood description of procedures andconceptual aspects of this invention. Each exemplified compound andintermediate was named using ACD/ChemSketch Version 12.5 (13 May 2009),Advanced Chemistry Development Inc., Toronto, Ontario), or ChemDraw®Ver. 9.0.5 (CambridgeSoft, Cambridge, Mass.).

Experimentals Example 12-{(4-fluorobenzyl)[4-(pyridin-3-yl)benzyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 9, substituting3-(4-(chloromethyl)phenyl)pyridine for 1-(2-chloroethyl)pyrrolidine.

Example 2N-[3-(1H-imidazol-1-yl)propyl]-2-{methyl[4-(pyridin-3-yl)benzyl]amino}-1,3-thiazole-5-carboxamideExample 2A methyl 2-(4-(pyridin-3-yl)benzylamino)thiazole-5-carboxylate

To a 250 mL round-bottomed flask was added 4-(pyridin-3-yl)benzaldehyde(4 g, 21.8 mmol), methyl 2-aminothiazole-5-carboxylate (3.45 g, 21.83mmol) and acetic acid (0.375 ml, 6.55 mmol) in toluene (109 ml). Thereaction mixture was heated at reflux under Dean-Stark conditions for 3hours, cooled to room temperature, and the volatiles were removed byrotary evaporation. Methanol was added, the solution was cooled to 0°C., and sodium borohydride (1.322 g, 34.9 mmol) was carefully added. Thereaction was stirred at 0° C. for 15 minutes and allowed to warm to roomtemperature while stirring for an additional 2 hour. The solids werefiltered off, washed with water and dried under high vacuum to give thetitle compound which was used in the next step without furtherpurification.

Example 2B 2-(methyl(4-(pyridin-3-yl)benzyl)amino)thiazole-5-carboxylicacid

Example 2A (500 mg, 1.537 mmol) was dissolved in tetrahydrofuran (7683μl) and sodium hydride (92 mg, 2.305 mmol) was added carefully. Thesuspension was allowed to stir for about 20 minutes at room temperature.Iodomethane (106 μl, 1.690 mmol) was then added and the reaction wasstirred for an additional 30 minutes. To the mixture was added excess 1Naqueous NaOH followed by additional methanol and stirred at 55° C. for1.5 hours. The reaction mixture was concentrated by rotary evaporationand the residue was taken up in water. The pH was adjusted to around 5-6by addition of 2 N aqueous HCl, upon which time white solidsprecipitated out and were collected by vacuum filtration. The solidswere washed with water, diethyl ether, and dried under high vacuumovernight to provide the title compound.

Example 2CN-[3-(1H-imidazol-1-yl)propyl]-2-{methyl[4-(pyridin-3-yl)benzyl]amino}-1,3-thiazole-5-carboxamide

To a 20 mL vial was added Example 2B (100 mg, 0.307 mmol) and3-(1H-imidazol-1-yl)propan-1-amine (40.3 μl, 0.338 mmol) in DMF (1229μl). 1-Ethyl-3-[3-(dimethylamino)propyl]-carbodiimide hydrochloride (103mg, 0.538 mmol) and 1-hydroxybenzotriazole hydrate (82 mg, 0.538 mmol)were added and the reaction mixture was stirred over the weekend at roomtemperature. The reaction mixture was purified directly by HPLC (0-70%water acetonitrile) to give the title compound. ¹H NMR (300 MHz,DMSO-d₆) δ 8.88 (d, J=1.8 Hz, 1H), 8.56 (dd, J=4.8, 1.5 Hz, 1H), 8.22(t, J=5.6 Hz, 1H), 8.10-8.00 (m, 1H), 7.80 (s, 1H), 7.72 (d, J=8.2 Hz,2H), 7.64 (s, 1H), 7.52-7.44 (m, 1H), 7.40 (d, J=8.2 Hz, 2H), 7.19 (s,1H), 6.88 (s, 1H), 4.79 (s, 2H), 3.99 (t, J=6.9 Hz, 2H), 3.20-3.11 (m,2H), 3.11 (s, 3H), 1.90 (p, J=6.9 Hz, 2H); MS (ESI(+)) m/e 433.13(M+H)⁺.

Example 32-[(4-fluorobenzyl)(methyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamideExample 3A methyl 2-(4-fluorobenzylamino)thiazole-5-carboxylate

The title compound was prepared as described in Example 2A, substituting4-fluorobenzaldehyde for 4-(pyridin-3-yl)benzaldehyde.

Example 3B 2-((4-fluorobenzyl)(methyl)amino)thiazole-5-carboxylic acid

The title compound was prepared as described in Example 2B, substitutingExample 3A for Example 2A.

Example 3C2-[(4-fluorobenzyl)(methyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide

The title compound was prepared as described in Example 2C, substitutingExample 3B for Example 2B. ¹H NMR (300 MHz, DMSO-d₆) δ 8.20 (t, J=5.6Hz, 1H), 7.78 (s, 1H), 7.63 (s, 1H), 7.37-7.28 (m, 2H), 7.22-7.13 (m,3H), 6.88 (t, J=1.1 Hz, 1H), 4.71 (bs, 2H), 3.99 (t, J=6.9 Hz, 2H),3.20-3.09 (m, 2H), 3.05 (s, 3H), 1.90 (p, J=6.9 Hz, 2H); MS (ESI(+)) m/e374.1 (M+H)⁺.

Example 62-[(4-fluorobenzyl)(3-methylbutanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamideExample 6A N-(3-(1H-imidazol-1-yl)propyl)-2-bromothiazole-5-carboxamide

2-Bromothiazole-5-carboxylic acid (0.4 g, 1.923 mmol),3-(1H-imidazole-1-yl)propan-1-amine (0.265 g, 2.115 mmol), andbenzotriazol-1-yloxytris(dimethylamino)phosphonium hexafluorophosphate(BOP) (0.935 g, 2.115 mmol) were mixed in dichloromethane (7 ml),treated with Hunig's base (0.705 ml, 4.04 mmol) and stirred at 25° C.for 2 hours. The reaction mixture was diluted with dichloromethane andwashed with water and brine. The organic layer was dried (MgSO₄),filtered and concentrated. Purification by flash chromatography (silicagel, 2-20% methanol/dichloromethane) afforded the title compound.

Example 6BN-(3-(1H-imidazol-1-yl)propyl)-2-((4-fluorobenzyl)amino)thiazole-5-carboxamide

Example 6A (2 g, 6.35 mmol) and (4-fluorophenyl)methanamine (0.794 g,6.35 mmol) in acetonitrile (10 ml) were stirred at 120° C. overnight.The reaction mixture was cooled, concentrated, taken into ethyl acetateand washed with saturated aqueous NaHCO₃ and brine. The combined aqueouslayers were extracted twice with ethyl acetate. The combined organicextracts were dried (MgSO₄) and filtered. The filtrate was concentrateduntil solid material precipitated. The mixture was filtered to providethe title compound.

Example 6C2-[(4-fluorobenzyl)(3-methylbutanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide

Example 6B (0.2 g, 0.556 mmol) was dissolved in dichloromethane (2.7 ml)and pyridine (0.3 ml) and was treated dropwise with a solution of3-methylbutanoyl chloride (0.102 ml, 0.835 mmol) in dichloromethane (0.5ml). The reaction mixture was stirred at 25° C. for 2 hours,concentrated, and purified using reverse phase HPLC (Phenomenex LunaC8(2) 5 um 100 Å AXIA column (30 mm×75 mm) run with a gradient ofacetonitrile (A) and 0.1% trifluoroacetic acid in water (B), at a flowrate of 50 mL/min (0-0.5 min 10% A, 0.5-7.0 min linear gradient 10-95%A, 7.0-10.0 min 95% A, 10.0-12.0 min linear gradient 95-10% A) to affordthe title compound. ¹H NMR (400 MHz, CDCl₃) δ 7.87 (s, 1H), 7.60 (s,1H), 7.19-7.07 (m, 3H), 7.07-6.97 (m, 3H), 5.89 (s, 1H), 5.47 (s, 2H),4.07 (t, J=6.9 Hz, 2H), 3.46 (q, J=6.6 Hz, 2H), 2.43 (d, J=6.8 Hz, 2H),2.36-2.19 (m, 1H), 2.19-2.04 (m, 2H), 0.93 (d, J=6.6 Hz, 6H); MS(ESI(+)) m/e 443.5 (M+H)⁺.

The following examples were prepared as described in Example 6,substituting the appropriate amine in Example 6B and the appropriateacyl chloride in Example 6C. Title compounds were purified by eitherflash chromatography (silica gel column eluting with a gradient of 0-10%methanol in dichloromethane) or reverse-phase HPLC (as described inExample 6C). Accordingly, some examples were isolated as trifluoroaceticacid salts.

EX NAME ¹H NMR DATA MS DATA 4 2-[(4- ¹H NMR (400 MHz, CDCl₃) δ 9.08(ESI(+)) fluorobenzyl)(tetrahydro- (s, 1H), 7.93 (s, 1H), 7.36 (d, J =m/e 486 2H-pyran-4- 14.1 Hz, 2H), 7.17-7.08 (m, 2H), (M + H)⁺ylacetyl)amino]-N-[3-(1H- 7.03 (t, J = 8.5 Hz, 2H), 6.76 (ddd,imidazol-1-yl)propyl]-1,3- J = 47.8, 25.3, 16.1 Hz, 1H), 5.47thiazole-5-carboxamide (s, 2H), 4.31 (d, J = 2.8 Hz, 2H), 3.93 (d, J =11.0 Hz, 2H), 3.50 (dd, J = 11.4, 5.8 Hz, 2H), 3.42 (t, J = 11.8 Hz,2H), 2.48 (d, J = 6.7 Hz, 2H), 2.27-2.20 (m, 2H), 1.65 (d, J = 11.2 Hz,2H), 1.30-1.14 (m, 2H). 5 2-[(cyclohexylacetyl)(4- ¹H NMR (400 MHz,CDCl₃) δ 9.00 (ESI(+)) fluorobenzyl)amino]-N-[3- (s, 1H), 7.95 (s, 1H),7.32 (d, J = m/e 484 (1H-imidazol-1-yl)propyl]- 17.1 Hz, 2H), 7.19-7.08(m, 2H), (M + H)⁺ 1,3-thiazole-5-carboxamide 7.02 (t, J = 8.6 Hz, 2H),6.77 (s, 1H), 5.46 (s, 2H), 4.29 (t, J = 6.5 Hz, 2H), 3.55-3.40 (m, 2H),2.42 (d, J = 6.7 Hz, 2H), 2.23 (d, J = 6.8 Hz, 2H), 2.19 (d, J = 6.4 Hz,1H), 1.71 (dd, J = 35.7, 15.8 Hz, 2H), 1.35-1.19 (m, 2H), 1.15 (d, J =12.4 Hz, 2H), 1.00 (t, J = 12.6 Hz, 2H), 0.87 (dd, J = 22.6, 10.6 Hz,2H). 11 2-[(4-cyanobenzoyl)(4- ¹H NMR (400 MHz, CDCl₃) δ 9.33 (ESI(+))fluorobenzyl)amino]-N-[3- (s, 1H), 8.05 (d, J = 6.3 Hz, 1H), m/e 489(1H-imidazol-1-yl)propyl]- 7.69 (d, J = 8.4 Hz, 2H), 7.47 (d, J = (M +H)+ 1,3-thiazole-5-carboxamide 8.3 Hz, 2H), 7.31 (s, 2H), 6.97- 6.89 (m,4H), 6.82-6.71 (m, 1H), 5.31 (s, 2H), 4.35 (d, J = 4.9 Hz, 2H), 3.49 (d,J = 5.9 Hz, 2H), 2.23 (dd, J = 7.9, 2.8 Hz, 2H). 122-[(3-chlorobenzoyl)(4- ¹H NMR (400 MHz, CDCl₃) δ 9.16 (ESI(+))fluorobenzyl)amino]-N-[3- (s, 1H), 8.00 (s, 1H), 7.51-7.44 m/e 498(1H-imidazol-1-yl)propyl]- (m, 1H), 7.38-7.32 (m, 4H), 7.01- (M + H)+1,3-thiazole-5-carboxamide 6.88 (m, 5H), 5.37 (s, 2H), 4.34 (t, J = 6.4Hz, 2H), 3.53-3.47 (m, 2H), 2.30-2.19 (m, 2H). 132-[(4-fluorobenzoyl)(4- ¹H NMR (400 MHz, CDCl₃) δ 9.20 (ESI(+))fluorobenzyl)amino]-N-[3- (s, 1H), 7.99 (s, 1H), 7.48-7.39 m/e 482(1H-imidazol-1-yl)propyl]- (m, 2H), 7.35 (d, J = 15.2 Hz, 2H), (M + H)+1,3-thiazole-5-carboxamide 7.12 (dt, J = 19.0, 8.6 Hz, 2H), 6.96 (qd, J= 8.7, 6.0 Hz, 4H), 5.39 (s, 2H), 4.34 (t, J = 6.5 Hz, 2H), 3.51 (dd, J= 11.6, 6.0 Hz, 2H), 2.31-2.19 (m, 2H). 24 2-[(4- ¹H NMR (400 MHz,CDCl₃) δ 7.88 (ESI(+)) fluorobenzyl)(methoxyace- (s, 1H), 7.61 (s, 1H),7.15 (dd, J = m/e 432 tyl)amino]-N-[3-(1H- 8.6, 5.2 Hz, 2H), 7.10 (s,1H), 7.03 (M + H)+ imidazol-1-yl)propyl]-1,3- (d, J = 8.6 Hz, 2H), 6.99(d, J = thiazole-5-carboxamide 8.1 Hz, 2H), 5.45 (s, 2H), 4.30- 4.24 (m,2H), 4.07 (t, J = 6.9 Hz, 2H), 3.48-3.43 (m, 5H), 2.18- 2.10 (m, 2H). 252-[(4-fluorobenzyl)(3- ¹H NMR (400 MHz, CDCl₃) δ 7.88 (ESI(+))methoxypropanoyl)amino]- (s, 1H), 7.60 (s, 1H), 7.16 (dd, J = m/e 446N-[3-(1H-imidazol-1- 8.6, 5.2 Hz, 2H), 7.10 (s, 1H), 7.04- (M + H)+yl)propyl]-1,3-thiazole-5- 6.99 (m, 2H), 6.98 (s, 1H), 5.92 carboxamide(s, 1H), 5.51 (s, 2H), 4.06 (t, J = 6.9 Hz, 2H), 3.75 (t, J = 6.2 Hz,2H), 3.48-3.41 (m, 2H), 3.33 (s, 3H), 2.81 (t, J = 6.2 Hz, 2H), 2.12(dd, J = 6.9, 3.9 Hz, 2H). 44 1-{2-[(4-fluorobenzyl)(5- (ESI(+)){[3-(1H-imidazol-1- m/e 480 yl)propyl]carbamoyl}-1,3- (M + H)+thiazol-2-yl)amino]-2- oxoethyl}pyridinium 45 2-{[2-(4- ¹H NMR (400 MHz,CDCl₃) δ 7.98 (ESI(+)) fluorophenyl)ethyl](3- (s, 1H), 7.58 (s, 1H),7.20-7.07 m/e 458 methylbutanoyl)amino}-N- (m, 3H), 7.07-6.95 (m, 3H),5.87 (M + H)+ [3-(1H-imidazol-1- (dd, J = 8.9, 3.5 Hz, 1H), 4.35 (t, J =yl)propyl]-1,3-thiazole-5- 7.3 Hz, 2H), 4.07 (t, J = 6.9 Hz, carboxamide2H), 3.46 (dd, J = 8.0, 4.8 Hz, 2H), 3.04 (t, J = 7.3 Hz, 2H), 2.21 (d,J = 6.7 Hz, 2H), 2.19-2.16 (m, 1H), 2.16-2.08 (m, 2H), 0.92 (d, J = 6.2Hz, 6H). 48 2-{[2-(4-cyanophenyl)ethyl](3- ¹H NMR (400 MHz, CDCl₃) δ9.09 (ESI(+)) methylbutanoyl)amino}-N- (s, 1H), 8.01 (s, 1H), 7.63 (d, J= m/e 465 [3-(1H-imidazol-1- 8.1 Hz, 2H), 7.37 (s, 1H), 7.33 (d, J =(M + H)+ yl)propyl]-1,3-thiazole-5- 7.9 Hz, 3H), 6.74 (s, 1H), 4.39 (t,carboxamide J = 7.4 Hz, 2H), 4.33 (t, J = 6.3 Hz, 2H), 3.51 (d, J = 5.4Hz, 2H), 3.20-3.07 (m, 2H), 2.31-2.21 (m, 5H), 0.95 (d, J = 6.4 Hz, 6H).49 2-{[2-(4-cyanophenyl)ethyl](tetra- ¹H NMR (400 MHz, CDCl₃) δ 9.12(ESI(+)) hydro-2H-pyran-4- (s, 1H), 8.00 (s, 1H), 7.63 (d, J = m/e 507ylacetyl)amino}-N-[3-(1H- 8.0 Hz, 2H), 7.39 (s, 1H), 7.33 (d, J = (M +H)+ imidazol-1-yl)propyl]-1,3- 8.2 Hz, 3H), 6.72 (s, 1H), 4.45-thiazole-5-carboxamide 4.25 (m, 4H), 3.97 (d, J = 8.2 Hz, 2H), 3.60-3.33(m, 4H), 3.14 (t, J = 7.3 Hz, 2H), 2.33 (d, J = 6.5 Hz, 4H), 1.65 (d, J= 12.9 Hz, 2H), 1.36-1.19 (m, 2H). 50 2-[(4-cyanobenzyl)(3- ¹H NMR (400MHz, CDCl₃) δ 9.21 (ESI(+)) methylbutanoyl)amino]-N- (dd, J = 17.5, 1.7Hz, 1H), 7.91 (d, m/e 451 [3-(1H-imidazol-1- J = 4.2 Hz, 1H), 7.64 (d, J= 8.3 (M + H)+ yl)propyl]-1,3-thiazole-5- Hz, 2H), 7.35 (d, J = 18.5 Hz,2H), carboxamide 7.24 (s, 1H), 7.04-6.89 (m, 1H), 5.53 (s, 2H), 4.34(dd, J = 9.6, 3.6 Hz, 2H), 3.57-3.43 (m, 2H), 2.38 (d, J = 6.7 Hz, 2H),2.29-2.19 (m, 3H), 0.93 (d, J = 6.6 Hz, 6H). 51 2-[(4- ¹H NMR (400 MHz,CDCl₃) δ 9.12 (ESI(+)) cyanobenzyl)(tetrahydro- (s, 1H), 8.00 (s, 1H),7.63 (d, J = m/e 493 2H-pyran-4- 8.0 Hz, 2H), 7.39 (s, 1H), 7.33 (d, J =(M + H)+ ylacetyl)amino]-N-[3-(1H- 8.2 Hz, 3H), 6.72 (s, 1H), 5.53imidazol-1-yl)propyl]-1,3- (s, 2H), 4.45-4.25 (m, 2H), 3.97thiazole-5-carboxamide (d, J = 8.2 Hz, 2H), 3.60-3.33 (m, 2H), 3.14 (t,J = 7.3 Hz, 2H), 2.33 (d, J = 6.5 Hz, 4H), 1.65 (d, J = 12.9 Hz, 2H),1.36-1.19 (m, 3H). 52 2-{[2-(4- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))cyanophenyl)ethyl](tetrahydro- δ 9.00 (s, 1H), 8.06 (s, 1H), 7.73 (s,m/e 493 furan-3-ylacetyl)amino}- 1H), 7.68 (d, J = 8.1 Hz, 2H), 7.59(M + H)+ N-[3-(1H-imidazol-1- (s, 1H), 7.41 (d, J = 8.1 Hz, 2H),yl)propyl]-1,3-thiazole-5- 4.47 (t, J = 7.2 Hz, 2H), 4.34 (t, J =carboxamide 6.9 Hz, 2H), 4.02-3.88 (m, 1H), 3.79 (dt, J = 8.1, 4.0 Hz,1H), 3.73 (dd, J = 15.5, 7.6 Hz, 1H), 3.41 (t, J = 6.4 Hz, 2H),3.27-3.23 (m, 1H), 3.19 (t, J = 7.2 Hz, 2H), 2.64 (d, J = 9.4 Hz, 2H),2.62-2.57 (m, 1H), 2.24-2.16 (m, 2H), 2.16- 2.08 (m, 1H), 1.47 (dd, J =12.6, 6.3 Hz, 1H). 53 2-[(4-fluorobenzyl)(3- ¹H NMR (400 MHz, CDCl₃) δ7.94 (ESI(+)) methylbutanoyl)amino]-N- (s, 1H), 7.31 (s, 1H), 7.25 (s,1H), m/e 458 [3-(2-methyl-1H-imidazol- 7.18-7.08 (m, 2H), 7.02 (t, J =(M + H)+ 1-yl)propyl]-1,3-thiazole-5- 8.5 Hz, 2H), 6.66 (s, 1H), 5.47(s, carboxamide 2H), 4.13 (t, J = 6.9 Hz, 2H), 3.52 (d, J = 5.9 Hz, 2H),2.68 (s, 3H), 2.44 (d, J = 6.8 Hz, 2H), 2.31- 2.22 (m, 1H), 2.14 (d, J =6.4 Hz, 2H), 0.93 (d, J = 6.6 Hz, 6H). 54 2-[(4-fluorobenzyl)(3- ¹H NMR(400 MHz, CDCl₃) δ 8.85 (ESI(+)) methylbutanoyl)amino]-N- (s, 1H), 7.95(d, J = 7.1 Hz, 1H), m/e 458 [3-(4-methyl-1H-imidazol- 7.11 (dd, J =8.5, 5.3 Hz, 2H), 7.00 (M + H)+ 1-yl)propyl]-1,3-thiazole-5- (dd, J =20.2, 11.7 Hz, 4H), 5.45 carboxamide (s, 2H), 4.21 (t, J = 6.6 Hz, 2H),3.55-3.40 (m, 2H), 2.45-2.38 (m, 2H), 2.32 (d, J = 5.6 Hz, 3H),2.29-2.23 (m, 1H), 2.21-2.15 (m, 2H), 0.92 (d, J = 6.6 Hz, 6H). 612-[(4- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))cyanobenzyl)(tetrahydrofuran- δ 8.99 (s, 1H), 7.94 (s, 1H), 7.74- m/e479 3-ylacetyl)amino]-N-[3- 7.70 (m, 3H), 7.58 (s, 1H), 7.36 (d, (M +H)+ (1H-imidazol-1-yl)propyl]- J = 8.1 Hz, 2H), 5.63 (d, J = 4.11,3-thiazole-5-carboxamide Hz, 2H), 4.32 (t, J = 6.9 Hz, 2H), 4.03-3.91(m, 1H), 3.81-3.67 (m, 2H), 3.42-3.32 (m, 3H), 2.84- 2.77 (m, 1H),2.76-2.69 (m, 2H), 2.26-2.09 (m, 3H), 1.61- 1.46 (m, 1H). 622-[(4-cyanobenzyl)(3- ¹H NMR (400 MHz, CDCl₃) δ 9.18 (ESI(+))methoxypropanoyl)amino]- (s, 1H), 7.91 (s, 1H), 7.63 (d, J = m/e 453N-[3-(1H-imidazol-1- 8.3 Hz, 2H), 7.36 (d, J = 18.0 Hz, (M + H)+yl)propyl]-1,3-thiazole-5- 2H), 7.28 (d, J = 8.3 Hz, 2H), 6.92carboxamide (s, 1H), 5.58 (s, 2H), 4.34 (t, J = 6.5 Hz, 2H), 3.76 (t, J= 6.0 Hz, 2H), 3.50 (d, J = 5.8 Hz, 2H), 3.33 (s, 3H), 2.77 (t, J = 6.0Hz, 2H), 2.32-2.18 (m, 2H). 74 2-[(4-fluorobenzoyl)(3- ¹H NMR (400 MHz,DMSO-d₆) δ (ESI(+)) methylbutyl)amino]-N-[3- 8.56 (t, J = 5.5 Hz, 1H),8.15 (s, m/e 444 (1H-imidazol-1-yl)propyl]- 1H), 7.72 (dd, J = 8.7, 5.3Hz, 3H), (M + H)+ 1,3-thiazole-5-carboxamide 7.39 (t, J = 8.9 Hz, 2H),7.23 (s, 1H), 6.92 (s, 1H), 4.04 (dd, J = 15.5, 8.6 Hz, 4H), 3.21 (dd, J= 12.8, 6.7 Hz, 2H), 1.97 (dd, J = 13.9, 6.9 Hz, 2H), 1.49 (dd, J =15.2, 7.1 Hz, 2H), 1.38 (dt, J = 13.2, 6.4 Hz, 1H), 0.67 (d, J = 6.5 Hz,6H). 75 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, DMSO- (ESI(+))yl)propyl]-2-[(3- d₆/D₂O) δ ppm 8.80 (s, 1 H) 7.98 m/e 442methoxypropanoyl)(4- (s, 1 H) 7.62 (s, 1 H) 7.49 (s, 1 H) (M + H)+methylbenzyl)amino]-1,3- 7.11-7.17 (m, 3 H) 7.04-7.07 (m,thiazole-5-carboxamide 2 H) 5.46 (s, 2 H) 4.24 (t, J = 7.02 Hz, 3 H)3.65 (t, J = 5.95 Hz, 2 H) 3.28-3.31 (m, 3 H) 2.86 (t, J = 5.95 Hz, 2 H)2.27 (s, 4 H) 2.06- 2.13 (m, 2 H). 76 N-(5-{[3-(1H-imidazol-1- ¹H NMR(400 MHz, CDCl₃) δ 9.16 (ESI(+)) yl)propy1]carbamoyl}-1,3- (s, 1H), 8.42(s, 1H), 8.08 (s, 1H), m/e 417 thiazol-2-yl)-N-(3- 7.35 (d, J = 13.4 Hz,2H), 7.24- (M + H)+ methylbutyl)-1,2-oxazole-5- 7.08 (m, 1H), 7.05 (s,1H), 4.45 (d, carboxamide J = 6.7 Hz, 2H), 4.36 (t, J = 6.4 Hz, 2H),3.55-3.49 (m, 2H), 2.28- 2.23 (m, 3H), 1.75-1.69 (m, 2H), 1.52 (dd, J =14.7, 7.1 Hz, 1H), 0.95 (d, J = 3.8 Hz, 6H). 77 N-[3-(1H-imidazol-1- ¹HNMR (500 MHz, DMSO- (ESI(+)) yl)propyl]-2-[(3- d₆/D₂O) δ 8.12 (s, 1H),7.68 (s, m/e 470 methylbutyl)(2- 1H), 7.33 (t, J = 8.0 Hz, 2H), 7.21(M + H)+ phenoxypropanoyl)amino]- (s, 1H), 7.01 (t, J = 7.4 Hz, 1H),1,3-thiazole-5-carboxamide 6.97 (d, J = 8.3 Hz, 2H), 6.91 (s, 1H), 5.58(q, J = 6.3 Hz, 1H), 4.24 (t, J = 9.8 Hz, 1H), 4.07 (d, J = 10.8 Hz,1H), 4.02 (t, J = 6.9 Hz, 2H), 3.20 (t, J = 6.9 Hz, 2H), 1.95 (p, J =6.9 Hz, 2H), 1.60 (dd, J = 11.9, 7.6 Hz, 1H), 1.56 (d, J = 6.3 Hz, 3H),1.51 (dd, J = 12.9, 6.5 Hz, 1H), 0.81 (dd, J = 28.5, 6.3 Hz, 6H). 852-{[2-(4- ¹H NMR (400 MHz, CDCl₃) δ 9.06 (ESI(+)) cyanophenyl)ethyl](3-(s, 1H), 7.99 (s, 1H), 7.62 (d, J = m/e 467 methoxypropanoyl)amino}- 8.2Hz, 2H), 7.39-7.33 (m, 4H), (M + H)+ N-[3-(1H-imidazol-1- 4.42 (s, 2H),4.32 (s, 2H), 3.75 (t, J = yl)propyl]-1,3-thiazole-5- 6.1 Hz, 2H), 3.51(d, J = 5.6 Hz, carboxamide 2H), 3.36 (s, 3H), 3.12-3.16 (m, 2H), 2.74(t, J = 6.1 Hz, 2H), 2.20- 2.25 (m, 2H). 93 N-[3-(1H-imidazol-1- ¹H NMR(400 MHz, DMSO- (ESI(+)) yl)propyl]-2-[(3- d₆/D₂O) δ ppm 8.72 (d, J =4.88 Hz, m/e 430 methoxypropanoyl)(pyrimidin- 2 H) 7.87 (s, 1 H) 7.59(s, 1 H) (M + H)+ 2-ylmethyl)amino]-1,3- 7.38 (t, J = 4.88 Hz, 1 H) 7.13(s, 1 thiazole-5-carboxamide H) 6.88 (s, 1 H) 5.65 (s, 2 H) 4.01 (t, J =7.02 Hz, 2 H) 3.69 (t, J = 6.26 Hz, 2 H) 3.21-3.25 (m, 5 H) 2.89 (t, J =6.26 Hz, 2 H) 1.93- 2.02 (m, 2 H). 94 N-[3-(1H-imidazol-1- ¹H NMR (400MHz, DMSO- (ESI(+)) yl)propyl]-2-{(3- d₆/D₂O) δ ppm 8.09 (d, J = 5.19Hz, m/e 459 methoxypropanoyl)[(2- 1 H) 7.96 (s, 1 H) 7.60 (s, 1 H) (M +H)+ methoxypyridin-4- 7.13 (s, 1H) 6.89 (s, 1H) 6.79 (s, 1yl)methyl]amino}-1,3- H) 6.51 (s, 1 H) 5.47 (s, 2 H) 4.02thiazole-5-carboxamide (t, J = 6.87 Hz, 2 H) 3.82-3.86 (m, 3 H) 3.66 (t,J = 5.95 Hz, 2 H) 3.22- 3.25 (m, 2 H) 3.21 (s, 3 H) 2.84 (t, J = 6.10Hz, 2 H) 1.98 (t, J = 7.02 Hz, 2 H). 95 N-[3-(1H-imidazol-1- ¹H NMR (400MHz, DMSO- (ESI(+)) yl)propyl]-2-[(3- d₆/D₂O) δ ppm 8.00 (s, 1 H), 7.60m/e 419 methoxypropanoyl)(1,3- (s, 1 H), 7.13 (s, 1 H), 6.89 (s, 1 H),(M + H)+ oxazol-4-ylmethyl)amino]- 5.36 (s, 1 H), 4.02 (t, 2 H), 3.50-1,3-thiazole-5-carboxamide 3.75 (m, 3 H), 3.22-3.25 (m, 4 H), 3.13 (t, J= 6.26 Hz, 2 H), 2.29- 2.40 (m, 1 H), 1.94-2.03 (m, 2 H). 962-{[(5-chloropyridin-2- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))yl)methyl](3- δ 8.97 (s, 1H), 8.46 (d, J = 2.4 Hz, m/e 463methoxypropanoyl)amino}- 1H), 7.90 (s, 1H), 7.80 (dd, J = 8.4, (M + H)+N-[3-(1H-imidazol-1- 2.5 Hz, 1H), 7.70 (d, J = 1.6 Hz,yl)propyl]-1,3-thiazole-5- 1H), 7.57 (s, 1H), 7.39 (d, J = 8.4carboxamide Hz, 1H), 5.60 (s, 2H), 4.31 (t, J = 6.9 Hz, 2H), 3.77 (t, J= 6.0 Hz, 2H), 3.38 (t, J = 6.3 Hz, 2H), 3.33 (s, 3H), 3.03 (t, J = 6.0Hz, 2H), 2.25-2.08 (m, 2H). 97 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz,DMSO- (ESI(+)) yl)propyl]-2-{(3- d₆/D₂O) δ ppm 8.31 (d, J = 4.88 m/e 443methoxypropanoyl)[(4- Hz, 1 H), 7.93-7.95 (m, 1 H), 7.89 (M + H)+methylpyridin-3- (s, 1 H), 7.60 (s, 1 H), 7.24 (d, J =yl)methyl]amino}-1,3- 4.88 Hz, 1 H), 7.13 (s, 1 H), 6.88thiazole-5-carboxamide (s, 1H), 5.48 (s, 1 H), 4.02 (t, J = 6.87 Hz, 2H), 3.67 (q, J = 6.31 Hz, 2 H), 3.22-3.24 (m, 2 H), 3.20 (s, 3 H), 2.85(t, J = 5.95 Hz, 2 H), 2.39 (s, 3 H), 1.94-2.02 (m, 2 H). 98N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, DMSO- (ESI(+)) yl)propyl]-2-{(3-d₆/D₂O) δ ppm 8.04 (d, J = 2.44 m/e 459 methoxypropanoyl)[(6- Hz, 1 H),8.00 (s, 1 H), 7.60 (s, 1 (M + H)+ methoxypyridin-3- H), 7.55 (dd, J =8.54, 2.44 Hz, 1 yl)methyl]amino}-1,3- H), 7.13 (s, 1 H), 6.89 (s, 1 H),thiazole-5-carboxamide 6.76 (d, J = 8.54 Hz, 1 H), 5.43 (s, 2 H), 4.02(t, J = 6.87 Hz, 2 H), 3.82-3.86 (m, 3 H), 3.68 (t, J = 6.10 Hz, 3 H),3.24 (d, J = 2.44 Hz, 2 H), 3.22 (s, 3 H), 2.90-2.95 (m, 2 H), 1.95-2.03(m, 2 H), 1.22 (s, 1 H). 99 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, DMSO-(ESI(+)) yl)propyl]-2-{(3- d₆/D₂O) δ ppm 8.80 (s, 1 H), 8.05 m/e 449methoxypropanoyl)[(4- (s, 1 H), 7.60 (s, 1 H), 7.14 (s, 1 H), (M + H)+methyl-1,3-thiazol-5- 6.89 (s, 1 H), 5.58 (s, 2 H), 4.02 (t,yl)methyl]amino}-1,3- J = 7.02 Hz, 2 H), 3.69 (t, J = 6.10thiazole-5-carboxamide Hz, 2 H), 3.22-3.25 (m, 5 H), 2.95 (t, J = 6.10Hz, 2 H), 2.46 (s, 3 H), 1.95-2.03 (m, 2 H). 100 2-{[2-(3- ¹H NMR (400MHz, DMSO- (ESI(+)) hydroxyphenyl)ethyl](3- d₆/D₂O) δ ppm 7.63 (s, 1 H),7.58- m/e 458 methoxypropanoyl)amino} 7.61 (m, 1 H), 7.33 (s, 1 H) 7.13(s, (M + H)+ N-[3-(1H-imidazol-1- 2 H), 6.94-6.99 (m, 1 H), 6.89 (s,yl)propyl]-1,3-thiazole-5- 1 H), 3.98-4.02 (m, 2 H), 3.69 (t,carboxamide J = 6.26 Hz, 2 H), 3.50 (s, 2 H), 3.30 (s, 3 H), 3.19 (t, J= 6.87 Hz, 2 H), 2.88-2.93 (m, 2 H), 2.76- 2.80 (m, 3 H), 1.93-1.97 (m,J = 6.41 Hz, 3 H). 101 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, DMSO-(ESI(+)) yl)propyl]-2-{(3- d₆/D₂O) δ ppm 8.49 (d, J = 4.88 Hz, m/e 443methoxypropanoyl)[2- 1 H), 8.03 (s, 1 H), 7.62-7.71 (m, (M + H)+(pyridin-2-yl)ethyl]amino}- 2 H), 7.21-7.25 (m, 2 H), 7.16 (s,1,3-thiazole-5-carboxamide 1 H), 6.91 (s, 1 H), 4.52-4.57 (m, acetate(1:1) 2 H), 4.04 (t, J = 6.87 Hz, 2 H), 3.64 (t, J = 6.26 Hz, 2 H),3.58- 3.62 (m, 1 H), 3.24 (s, 3 H), 3.17- 3.21 (m, 3 H), 2.84 (t, J =6.26 Hz, 2 H), 1.96-2.04 (m, 2 H), 1.92 (s, 1 H). 1022-{[2-(l,3-benzodioxol-5- ¹H NMR (400 MHz, DMSO- (ESI(+)) yl)ethyl](3-d₆/D₂O) δ ppm 8.06 (s, 1 H), 7.61 m/e 486 methoxypropanoyl)amino}- (s, 1H), 7.14 (s, 1 H), 6.89 (s, 1 H), (M + H)+ N-[3-(1H-imidazol-1- 6.79 (d,J = 7.93 Hz, 1 H), 6.76 (d, yl)propyl]-1,3-thiazole-5- J = 1.53 Hz, 1H), 6.65 (dd, J = carboxamideacetate (1:1) 7.93, 1.53 Hz, 1 H), 5.93 (s,2 H), 4.34-4.3 8 (m, 2 H), 4.03 (t, J = 7.02 Hz, 2 H), 3.62 (t, J = 6.26Hz, 2 H), 3.26-3.27 (m, 2 H), 3.24 (s, 3 H), 2.94 (t, J = 7.32 Hz, 2 H),2.77 (t, J = 6.26 Hz, 2 H), 1.96- 2.06 (m, 1 H), 1.88 (s, 1 H). 1032-{[2-(4- ¹H NMR (400 MHz, DMSO- (ESI(+)) chlorophenyl)ethyl](3- d₆/D₂O)δ ppm 8.05 (s, 1 H), 7.61 m/e 476 methoxypropanoyl)amino}- (s, 1 H),7.31-7.34 (m, 2 H), 7.23 (M + H)+ N-[3-(1H-imidazol-1- (d, 2 H), 7.14(s, 1 H), 6.89 (s, 1 yl)propyl]-1,3-thiazole-5- H), 4.37-4.42 (m, 2 H),4.03 (t, J = carboxamideacetate (1:1) 7.02 Hz, 2 H), 3.63 (t, J = 6.26Hz, 2 H), 3.25 (s, 2 H), 3.24 (s, 3 H), 3.02 (t, J = 7.32 Hz, 2 H), 2.79(t, J = 6.26 Hz, 2 H), 1.96-2.04 (m, 2 H), 1.88 (s, 1 H). 1042-{[2-(3-fluorophenyl)ethyl](3- ¹H NMR (400 MHz, DMSO- (ESI(+))methoxypropanoyl)amino}- d₆/D₂O) δ ppm 8.06 (s, 1 H), 7.61 m/e 460N-[3-(1H-imidazol-1- (s, 1 H), 7.30-7.37 (m, 1 H), 7.14 (M + H)+yl)propyl]-1,3-thiazole-5- (s, 1 H), 6.99-7.08 (m, 3 H), 6.90carboxamideacetate (1:1) (s, 1 H), 4.40-4.44 (m, 2 H), 4.03 (t, J = 7.02Hz, 2 H), 3.63 (t, J = 6.26 Hz, 2 H), 3.25 (s, 2 H), 3.24 (s, 3 H), 3.05(t, J = 7.48 Hz, 2 H), 2.80 (t, J = 6.10 Hz, 2 H), 1.96- 2.04 (m, 2 H),1.90 (s, 1 H). 105 2-{[2-(4- ¹H NMR (400 MHz, DMSO- (ESI(+))hydroxyphenyl)ethyl](3- d₆/D₂O) δ ppm 7.59-7.63 (m, 2 m/e 458methoxypropanoyl)amino}- H), 7.27 (d, J = 8.24 Hz, 2 H), 7.13 (M + H)+N-[3-(1H-imidazol-1- (s, 1 H), 7.00-7.04 (m, 2 H), 6.89yl)propyl]-1,3-thiazole-5- (s, 1 H), 4.00 (t, J = 7.02 Hz, 2 H),carboxamideacetate (1:1) 3.69 (t, J = 6.10 Hz, 2 H), 3.50 (t, J = 7.17Hz, 2 H), 3.30 (s, 2 H), 3.17- 3.24 (m, 3 H), 2.89 (t, J = 7.17 Hz, 2H), 2.77 (t, J = 6.26 Hz, 2 H), 1.96 (q, J = 7.12 Hz, 2 H), 1.85 (s, 2H). 106 2-{[2-(3-chlorophenyl)ethyl](3- ¹H NMR (400 MHz, DMSO- (ESI(+))methoxypropanoyl)amino}- d₆/D₂O) δ ppm 8.06 (s, 1 H), 7.62 m/e 476N-[3-(1H-imidazol-1- (s, 1 H), 7.23-7.34 (m, 3 H), 7.14- (M + H)+yl)propyl]-1,3-thiazole-5- 7.19 (m, 2 H), 6.90 (s, 1 H), 4.39-carboxamideacetate (1:1) 4.44 (m, 2 H), 4.03 (t, J = 6.87 Hz, 2 H), 3.63(t, J = 6.26 Hz, 2 H), 3.22-3.26 (m, 5 H), 3.04 (t, J = 7.32 Hz, 2 H),2.81 (t, J = 6.26 Hz, 2 H), 1.96-2.04 (m, 2 H), 1.92 (s, 1 H). 107N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, DMSO- (ESI(+))yl)propyl]-2-{[2-(3- d₆/D₂O) δ ppm 8.07 (s, 1 H), 7.61 m/e 472methoxyphenyl)ethyl](3- (s, 1 H), 7.21 (t, J = 7.78 Hz, 1 H), (M + H)+methoxypropanoyl)amino}- 7.14 (s, 1 H), 6.90 (s, 1 H), 6.75-1,3-thiazole-5-carboxamide 6.82 (m, 3 H), 4.40 (t, J = 7.32 Hz, acetate(1:1) 2 H), 4.03 (t, J = 7.02 Hz, 2 H), 3.73 (s, 3 H), 3.60 (t, J = 6.10Hz, 2 H), 3.24 (s, 2 H), 3.23 (s, 3 H), 2.99 (t, J = 7.32 Hz, 2 H), 2.74(t, J = 6.26 Hz, 2 H), 1.96-2.05 (m, 2 H), 1.91 (s, 1 H). 108 2-{[2-(2-¹H NMR (400 MHz, DMSO- (ESI(+)) fluorophenyl)ethyl](3- d₆/D₂O) δ ppm8.03 (s, 1 H), 7.61 m/e 460 methoxypropanoyl)amino}- (s, 1 H), 7.25-7.31(m, 2 H), 7.08- (M + H)+ N-[3-(1H-imidazol-1- 7.15 (m, 3 H), 6.90 (s, 1H), 4.43 yl)propyl]-1,3-thiazole-5- (t, J = 7.32 Hz, 2 H), 4.03 (t, J =carboxamide acetate (1:1) 6.87 Hz, 2 H), 3.62 (t, J = 6.26 Hz, 2 H),3.25 (s, 2 H), 3.23 (s, 3 H), 3.08 (t, J = 7.17 Hz, 2 H), 2.78 (t, J =6.26 Hz, 2 H), 1.96-2.03 (m, 2 H), 1.90 (s, 1 H). 1092-{[2-hydroxy-2-(4- ¹H NMR (400 MHz, DMSO- (ESI(+))methoxyphenyl)ethyl](3- d₆/D₂O) δ ppm 7.63 (s, 1 H), 7.59 m/e 488methoxypropanoyl)amino}- (s, 1 H), 7.29 (d, J = 8.85 Hz, 2 H), (M + H)+N-[3-(1H-imidazol-1- 7.13 (s, 1 H), 6.88-6.94 (m, 3 H),yl)propyl]-1,3-thiazole-5- 5.89 (t, J = 6.41 Hz, 1 H), 4.00 (t, J =carboxamide acetate (1:1) 7.02 Hz, 2 H), 3.76 (s, 3 H), 3.63 (d, J =6.41 Hz, 2H), 3.56 (t, J = 6.41 Hz, 2 H), 3.22 (s, 1 H), 3.20 (s, 3 H),3.17-3.19 (m, 1 H), 2.54- 2.57 (m, 2 H), 1.91-1.99 (m, 2 H), 1.86 (s, 1H). 110 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, DMSO- (ESI(+))yl)propyl]-2-{(3- d₆/D₂O) δ ppm 8.95 (s, 1 H), 8.47 m/e 443methoxypropanoyl)[1- (s, 1 H), 7.94 (d, J = 14.04 Hz, 1 (M + H)+(pyridin-2-yl)ethyl]amino}- H), 7.73-7.81 (m, 1 H), 7.68 (d, J =1,3-thiazole-5-carboxamide 4.88 Hz, 1 H), 7.56 (d, J = 1.83 Hz, 1 H),7.40 (d, J = 7.93 Hz, 1 H), 7.28 (d, J = 5.19 Hz, 1 H), 6.07- 6.14 (m,1H), 4.26 (q, J = 7.02 Hz, 3 H), 3.60-3.69 (m, 3 H), 3.20 (s, 3 H), 2.71(t, J = 6.26 Hz, 2 H), 2.05-2.15 (m, 3 H), 1.82 (d, J = 7.32 Hz, 3 H).111 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, DMSO- (ESI(+))yl)propyl]-2-{(3- d₆/D₂O) δ ppm 8.96 (d, J = 6.10 Hz, m/e 432methoxypropanoyl)[(1- 1 H), 8.08 (d, J = 27.77 Hz, 1 H), (M + H)+methyl-1H-pyrazol-4- 7.69 (d, J = 4.88 Hz, 1 H), 7.56-yl)methyl]amino}-1,3- 7.59 (m, 1 H), 7.49 (s, 1 H), 7.27thiazole-5-carboxamide (s, 1H), 5.28 (s, 1 H), 4.24-4.32 (m, 4 H),4.24-4.31 (m, 4 H), 3.75- 3.79 (m, 4 H), 3.70 (t, J = 6.10 Hz, 1 H),3.61 (t, J = 6.41 Hz, 1 H), 3.25 (s, 2 H), 3.23 (s, 2 H), 3.00 (t, J =6.10 Hz, 1 H), 2.61 (t, 1 H), 2.11 (m, 1 H). 1122-[(2,6-difluorobenzyl)(3- ¹H NMR (400 MHz, DMSO- (ESI(+))methoxypropanoyl)amino]- d₆/D₂O) δ ppm 8.70 (s, 1 H), 7.93 m/e 461N-[3-(1H-imidazol-1- (s, 1 H), 7.58 (s, 1 H), 7.43 (s, 1 H), (M + H)+yl)propyl]-1,3-thiazole-5- 7.36 (s, 1 H), 7.01 (t, J = 8.54 Hz, 2carboxamide H), 5.53 (s, 2 H), 4.21 (t, J = 7.02 Hz, 2 H), 3.70 (t, J =6.10 Hz, 2 H), 3.24 (s, 3 H), 2.99 (t, J = 6.26 Hz, 2 H), 2.03-2.10 (m,2 H), 1.10 (td, 3 H). 113 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, DMSO-(ESI(+)) yl)propyl]-2-{(3- d₆/D₂O) δ ppm 8.95 (s, 1 H), 8.35 m/e 443methoxypropanoyl)[(6- (s, 1 H), 7.98 (s, 1 H), 7.68 (d, J = (M + H)+methylpyridin-3- 1.83 Hz, 1 H), 7.62 (dd, J = 8.24,yl)methyl]amino}-1,3- 2.14 Hz, 1 H), 7.56 (s, 1 H), 7.32thiazole-5-carboxamide (d, J = 8.24 Hz, 1 H), 5.50 (s, 2 H), 4.26 (t, J= 7.17 Hz, 2 H), 3.65- 3.70 (m, 3 H), 3.22 (s, 3 H), 2.92 (t, J = 5.95Hz, 2 H), 2.48 (s, 3 H), 2.10 (q, J = 6.92 Hz, 3 H). 1142-[(4-chlorobenzyl)(3- ¹H NMR (400 MHz, DMSO- (ESI(+))methoxypropanoyl)amino]- d₆/D₂O) δ ppm 8.85 (s, 1 H), 7.97 m/e 462N-[3-(1H-imidazol-1- (s, 1 H), 7.64 (s, 1 H), 7.51 (s, 1 H), (M + H)+yl)propyl]-1,3-thiazole-5- 7.37 (d, J = 8.24 Hz, 2 H), 7.20 (d,carboxamide J = 8.54 Hz, 2 H), 5.49 (s, 2 H), 4.24 (t, J = 7.17 Hz, 2H), 3.66 (t, J = 5.95 Hz, 2 H), 3.28-3.30 (m, 2 H), 3.20 (s, 3 H), 2.86(t, J = 6.10 Hz, 2 H), 2.06-2.14 (m, 2 H). 115 N-[3-(1H-imidazol-1- ¹HNMR (400 MHz, DMSO- (ESI(+)) yl)propyl]-2-{(3- d₆/D₂O) δ ppm 8.96 (s, 1H), 8.52 m/e 444 methoxypropanoyl)[(5- (s, 1 H), 8.40 (s, 1 H), 7.92 (s,1 H), (M + H)+ methylpyrazin-2- 7.68 (s, 1 H), 7.56 (s, 1 H), 5.56 (s,yl)methyl]amino}-1,3- 2 H), 4.25 (t, J = 7.02 Hz, 2 H),thiazole-5-carboxamide 3.70 (t, J = 6.26 Hz, 2 H), 3.18- 3.25 (m, 5 H),3.02 (t, J = 6.10 Hz, 2 H), 2.46 (s, 3 H), 2.06-2.13 (m, 2 H). 1162-[(3-chlorobenzyl)(3- ¹H NMR (400 MHz, DMSO- (ESI(+))methoxypropanoyl)amino]- d₆/D₂O) δ ppm 8.72 (s, 1 H), 7.98 m/e 462N-[3-(1H-imidazol-1- (s, 1 H), 7.59 (s, 1 H), 7.45 (s, 1 H), (M + H)+yl)propyl]-1,3-thiazole-5- 7.37 (t, J = 7.78 Hz, 2 H), 7.22 (s, 1carboxamide H), 7.12-7.16 (m, 1 H), 5.50 (s, 2 H), 4.22 (t, J = 7.02 Hz,2 H), 3.66 (t, J = 6.10 Hz, 2 H), 3.28-3.30 (m, 2 H), 3.20 (s, 3 H),2.87 (t, J = 5.95 Hz, 2 H), 2.08 (q, J = 6.92 Hz, 2 H). 117N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, DMSO- (ESI(+)) yl)propyl]-2-{(3-d₆/D₂O) δ ppm 8.97 (s, 1 H), 8.30 m/e 443 methoxypropanoyl)[(5- (s, 1H), 7.92 (s, 1 H), 7.69 (s, 1 H), (M + H)+ methylpyridin-2- 7.56-7.61(m, 2 H), 7.22 (d, J = yl)methyl]amino}-1,3- 7.93 Hz, 1 H), 5.52 (s, 1H), 4.26 thiazole-5-carboxamide (t, J = 6.87 Hz, 2 H), 3.68 (t, J = 6.26Hz, 2 H), 3.26 (s, 2 H), 3.23 (s, 3 H), 2.95 (t, J = 6.26 Hz, 2 H), 2.27(s, 3 H), 2.05-2.15 (m, 2 H). 118 2-[(2,5-difluorobenzyl)(3- ¹H NMR (400MHz, DMSO- (ESI(+)) methoxypropanoyl)amino]- d₆/D₂O) δ ppm 8.73 (s, 1H), 7.59 m/e 464 N-[3-(1H-imidazol-1- (s, 1 H), 7.45 (s, 1 H) 7.21-7.28(M + H)+ yl)propyl]-1,3-thiazole-5- (m, J = 4.88 Hz, 1 H), 7.05-7.17carboxamide (m, 2 H), 6.83 (s, 1 H), 5.50 (s, 2 H), 4.22 (t, J = 6.87Hz, 2 H), 3.69 (t, J = 5.95 Hz, 2 H), 3.29 (t, 1 H), 3.24 (s, 1 H), 3.22(s, 3 H), 2.91 (t, J = 6.10 Hz, 2 H), 2.05-2.12 (m, 2 H). 119N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, DMSO- (ESI(+)) yl)propyl]-2-[(3-d₆/D₂O) δ ppm 8.92 (s, 1 H), 7.67 m/e 442 methoxypropanoyl)(2- (s, 1 H),7.54 (s, 1 H), 7.21-7.25 (M + H)+ methylbenzyl)amino]-1,3- (m, 1 H),7.14-7.19 (m, 2 H), 7.05- thiazole-5-carboxamide 7.11 (m, 1H), 6.68 (d,J = 7.63 Hz, 1 H), 5.45 (s, 2 H), 4.26 (t, J = 6.87 Hz, 2 H), 3.65 (t, J= 6.10 Hz, 2 H), 3.19 (s, 3 H), 2.80 (t, J = 6.10 Hz, 2 H), 2.37 (s, 3H), 2.28 (d, J = 5.49 Hz, 2 H), 2.03-2.14 (m, 2 H). 120N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, DMSO- (ESI(+)) yl)propyl]-2-[(3-d₆/D₂O) δ ppm 8.94 (s, 1 H), 7.68 m/e 442 methoxypropanoyl)(3- (s, 1 H),7.56 (s, 1 H), 7.21 (t, J = (M + H)+ methylbenzyl)amino]-1,3- 7.63 Hz, 1H), 7.02-7.10 (m, 2 thiazole-5-carboxamide H), 7.00 (s, 1 H), 6.93 (d, J= 7.63 Hz, 1 H), 5.48 (s, 2 H), 4.21-4.29 (m, 2 H), 3.65 (t, J = 6.10Hz, 2 H), 3.29-3.31 (m, 2 H), 3.20 (s, 3 H), 2.86 (t, J = 6.10 Hz, 2 H),2.26 (s, 3 H), 2.06-2.15 (m, 2 H). 121 N-[3-(1H-imidazol-1- ¹H NMR (400MHz, DMSO- (ESI(+)) yl)propyl]-2-[(3- d₆/D₂O) δ ppm 8.96 (s, 1 H), 8.47m/e 429 methoxypropanoyl)(pyridin- (d, 1 H), 7.92 (s, 1 H), 7.72-7.79(M + H)+ 2-ylmethyl)amino]-1,3- (m, 1 H), 7.69 (d, J = 1.53 Hz, 1 H),thiazole-5-carboxamide 7.57 (d, J = 1.83 Hz, 1 H), 7.26- 7.34 (m, 2 H),5.57 (s, 2 H), 4.26 (t, J = 6.87 Hz, 2 H), 3.68 (t, J = 5.95 Hz, 2 H),3.26 (s, 2 H), 3.22 (s, 3 H), 2.95 (t, J = 6.26 Hz, 2 H), 2.06- 2.14 (m,J = 13.35, 6.60, 6.60 Hz, 2 H). 122 N-[3-(1H-imidazol-1- ¹H NMR (400MHz, DMSO- (ESI(+)) yl)propyl]-2-[(3- d₆/D₂O) δ ppm 8.95 (s, 1 H), 8.45-m/e 429 methoxypropanoyl)(pyridin- 8.51 (m, 2 H), 7.98 (s, 1 H), 7.68(M + H)+ 3-ylmethyl)amino]-1,3- (s, 1 H), 7.64 (d, 1 H), 7.56 (s, 1thiazole-5-carboxamide H), 7.40 (d, J = 4.88 Hz, 1 H), 5.53 (s, 2 H),4.26 (t, J = 7.17 Hz, 2 H), 3.68 (t, J = 6.10 Hz, 2 H), 3.29- 3.31 (m, 2H), 3.21 (s, 3 H), 2.91 (t, J = 5.95 Hz, 2 H), 2.07-2.14 (m, 2 H). 133N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, CDCl₃) δ 9.07 (ESI(+))yl)propyl]-2-{(3- (s, 1H), 8.00 (s, 1H), 7.35 (d, J = m/e 470methylbutyl)[(2R)-2- 8.9 Hz, 2H), 7.30 (t, J = 8.0 Hz, (M + H)+phenoxypropanoyl]amino}- 2H), 7.01 (t, J = 7.4 Hz, 1H), 6.891,3-thiazole-5-carboxamide (d, J = 8.0 Hz, 3H), 5.23 (d, J = 6.4 Hz,1H), 4.31 (t, J = 6.5 Hz, 3H), 4.14 (t, J = 11.2 Hz, 1H), 3.48 (dd, J =10.8, 5.2 Hz, 2H), 2.25- 2.16 (m, 3H), 1.70 (d, J = 6.5 Hz, 3H), 1.63(m, 2H), 0.90 (dd, J = 5.8, 3.4 Hz, 6H). 134 N-[3-(1H-imidazol-1- ¹H NMR(400 MHz, CDCl₃) δ 9.06 (ESI(+)) yl)propyl]-2-{(3- (s, 1H), 8.00 (s,1H), 7.35 (d, J = m/e 470 methylbutyl)[(2S)-2- 9.8 Hz, 2H), 7.30 (t, J =8.0 Hz, (M + H)+ phenoxypropanoyl]amino}- 2H), 7.01 (t, J = 7.3 Hz, 1H),6.90 1,3-thiazole-5-carboxamide (d, J = 8.1 Hz, 2H), 6.77 (s, 1H), 5.23(d, J = 6.3 Hz, 1H), 4.30 (t, J = 6.5 Hz, 3H), 4.16 (s, 1H), 3.49 (dd, J= 10.8, 5.2 Hz, 2H), 2.24- 2.17 (m, 3H), 1.70 (d, J = 6.5 Hz, 3H), 1.63(m, 2H), 0.90 (dd, J = 5.9, 3.2 Hz, 6H). 135 N-(5-{[3-(1H-imidazol-1- ¹HNMR (400 MHz, CDCl₃) δ 9.13 (ESI(+)) yl)propy1]carbamoyl}-1,3- (s, 1H),8.08 (s, 1H), 7.35 (d, J = m/e 431 thiazol-2-yl)-5-methyl-N-(3- 9.6 Hz,2H), 7.12 (s, 1H), 6.44 (s, (M + H)+ methylbutyl)-1,2-oxazole-3- 1H),4.61-4.49 (m, 2H), 4.35 (t, J = carboxamide 6.5 Hz, 2H), 3.51 (d, J =5.6 Hz, 2H), 2.54 (s, 3H), 2.29-2.20 (m, 2H), 1.70-1.61 (m, 3H), 0.90(d, J = 6.0 Hz, 6H). 136 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, CDCl₃) δ9.06 (ESI(+)) yl)propyl]-2-[(3- (s, 1H), 7.99 (s, 1H), 7.36-7.28 m/e 456methylbutyl)(phenoxyace- (m, 4H), 7.03 (t, J = 7.3 Hz, 2H), (M + H)+tyl)amino]-1,3-thiazole-5- 6.94 (d, J = 8.3 Hz, 2H), 4.99 (s,carboxamide 2H), 4.30 (t, J = 6.5 Hz, 2H), 4.24- 4.08 (m, 2H), 3.47 (d,J = 5.6 Hz, 2H), 2.23-2.18 (m, 2H), 1.76- 1.63 (m, 3H), 0.99 (d, J = 6.2Hz, 6H). 137 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, CDCl₃) δ 9.07(ESI(+)) yl)propyl]-2-[(3- (s, 1H), 7.98 (s, 1H), 7.36 (d, J = m/e 454methylbutyl)(3- 3.5 Hz, 2H), 7.34-7.29 (m, 2H), (M + H)+phenylpropanoyl)amino]- 7.26-7.17 (m, 3H), 6.90 (s, 1H),1,3-thiazole-5-carboxamide 4.32 (t, J = 6.5 Hz, 2H), 4.18- 4.05 (m, 2H),3.50 (d, J = 5.8 Hz, 2H), 3.10 (t, J = 7.5 Hz, 2H), 2.97- 2.92 (m, 2H),2.27-2.19 (m, 2H), 1.66 (dt, J = 12.9, 6.4 Hz, 1H), 1.53 (dd, J = 16.0,7.1 Hz, 2H), 0.95 (d, J = 6.6 Hz, 6H). 138 N-[3-(1H-imidazol-1- ¹HNMR(400 MHz, CDCl₃) δ 9.06 (ESI (+)) yl)propyl]-2-[(3- (s, 1H), 7.96 (s,1H), 7.36 (dd, J = m/e 454 methylbutyl)(2- 11.5, 7.2 Hz, 4H), 7.29 (d, J= 7.2 (M + H)+ phenylpropanoyl)amino]- Hz, 1H), 7.24 (s, 2H), 6.62 (s,1H), 1,3-thiazole-5-carboxamide 4.31 (t, J = 6.5 Hz, 2H), 4.20 (dt, J =15.7, 8.4 Hz, 1H), 4.10 (q, J = 6.9 Hz, 1H), 3.94 (dt, J = 10.3, 7.4 Hz,1H), 3.50 (d, J = 5.9 Hz, 2H), 2.25-2.18 (m, 2H), 1.63-1.58 (m, 1H),1.57 (d, J = 6.8 Hz, 3H), 1.45 (dd, J = 15.8, 7.3 Hz, 2H), 0.93 (dd, J =19.8, 6.6 Hz, 6H). 139 2-{[(4- ¹HNMR (400 MHz, CDCl₃) δ 9.04 (ESI (+))fluorophenyl)acetyl](3- (s, 1H), 7.97 (s, 1H), 7.33 (d, J = m/e 458methylbutyl)amino}-N-[3- 9.4 Hz, 2H), 7.24 (dd, J = 8.4, 5.3 (M + H)+(1H-imidazol-1-yl)propyl]- Hz, 2H), 7.06 (t, J = 8.6 Hz, 2H),1,3-thiazole-5-carboxamide 6.78 (s, 1H), 4.29 (t, J = 6.2 Hz, 2H),4.24-4.12 (m, 2H), 3.97 (s, 2H), 3.48 (d, J = 5.4 Hz, 2H), 2.23- 2.18(m, 2H), 1.71 (dt, J = 13.1, 6.6 Hz, 1H), 1.65-1.58 (m, 2H), 0.99 (d, J= 6.5 Hz, 6H). 150 N-[3-(1H-imidazol-1- ¹HNMR (400 MHz, methanol-d₄)(ESI (+)) yl)propyl]-2-[(3- 88.98 (s, 1H), 8.01 (s, 1H), 7.71 (s, m/e408 methoxypropanoyl)(3- 1H), 7.57 (s, 1H), 4.33 (t, J = 6.9 (M + H)+methylbutyl)amino]-1,3- Hz, 2H), 4.30-4.23 (m, 2H), 3.79thiazole-5-carboxamide (t, J = 5.9 Hz, 2H), 3.39 (t, J = 6.4 Hz, 2H),3.36 (s, 3H), 2.97 (t, J = 5.9 Hz, 2H), 2.18 (p, J = 6.7 Hz, 2H), 1.72(dt, J = 13.1, 6.7 Hz, 1H), 1.68-1.59 (m, 2H), 1.00 (d, J = 6.5 Hz, 6H).151 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))yl)propyl]-2- δ 8.98 (s, 1H), 8.03 (s, 1H), 7.71 (s, m/e 394[(methoxyacetyl)(3- 1H), 7.57 (s, 1H), 4.49 (s, 2H), (M + H)+methylbutyl)amino]-1,3- 4.33 (t, J = 6.8 Hz, 2H), 4.19-thiazole-5-carboxamide 4.07 (m, 2H), 3.49 (s, 3H), 3.40 (t, J = 6.4 Hz,2H), 2.19 (p, J = 6.6 Hz, 2H), 1.71 (dt, J = 12.8, 6.5 Hz, 1H),1.67-1.56 (m, 2H), 1.00 (d, J = 6.4 Hz, 6H). 1522-[(cyclopropylcarbonyl)(3- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))methylbutyl)amino]-N-[3- δ 8.97 (s, 1H), 8.00 (s, 1H), 7.70 (t, m/e 390(1H-imidazol-1-yl)propyl]- J = 1.6 Hz, 1H), 7.56 (t, J = 1.6 (M + H)+1,3-thiazole-5-carboxamide Hz, 1H), 4.53-4.41 (m, 2H), 4.32 (t, J = 6.8Hz, 2H), 3.39 (t, J = 6.4 Hz, 2H), 2.28-2.10 (m, 3H), 1.81- 1.63 (m,3H), 1.16-1.04 (m, 4H), 1.01 (d, J = 6.2 Hz, 6H). 153(2S)-1-[(5-{[3-(1H- ¹H NMR (400 MHz, methanol-d₄) (ESI(+)) imidazol-1- δ8.97 (s, 1H), 8.03 (s, 1H), 7.71 (s, m/e 436 yl)propy1]carbamoyl}-1,3-1H), 7.57 (s, 1H), 5.50 (q, J = 6.8 (M + H)+ thiazol-2-yl)(3- Hz, 1H),4.53 (s, 1H), 4.33 (t, J = methylbutyl)amino]-1- 6.8 Hz, 2H), 4.04-3.91(m, 1H), oxopropan-2-yl acetate 3.39 (dd, J = 6.9, 5.6 Hz, 2H), 2.19 (p,J = 6.6 Hz, 2H), 2.12 (s, 3H), 1.80 (d, J = 5.4 Hz, 1H), 1.72 (dt, J =11.2, 6.2 Hz, 2H), 1.54 (d, J = 6.8 Hz, 3H), 1.00 (dd, J = 6.1, 2.0 Hz,6H). 154 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))yl)propyl]-2-[(3- δ 10.13 (d, J = 1.5 Hz, 1H), 8.98 m/e 448methylbutyl)(tetrahydro-2H- (s, 1H), 8.01 (s, 1H), 7.71 (s, 1H), (M +H)+ pyran-4-ylacetyl)amino]- 7.57 (s, 1H), 4.32 (t, J = 6.9 Hz,1,3-thiazole-5-carboxamide 2H), 4.28-4.19 (m, 2H), 3.94 (dd, J = 11.4,3.5 Hz, 2H), 3.47 (t, J = 11.0 Hz, 2H), 3.39 (t, J = 6.5 Hz, 2H), 2.67(d, J = 6.7 Hz, 2H), 2.19 (dd, J = 13.3, 6.7 Hz, 3H), 1.73 (dd, J =13.3, 6.4 Hz, 3H), 1.61 (dd, J = 15.7, 7.1 Hz, 2H), 1.39 (dd, J = 12.9,4.3 Hz, 2H), 1.01 (d, J = 6.5 Hz, 6H). 155 N-[3-(1H-imidazol-1- ¹H NMR(400 MHz, methanol-d₄) (ESI(+)) yl)propyl]-2-[(3- δ 8.98 (s, 1H), 8.02(s, 1H), 7.71 (s, m/e 420 methylbutyl)(tetrahydrofuran- 1H), 7.57 (s,1H), 4.31 (dt, J = (M + H)+ 3-ylcarbonyl)amino]-1,3- 15.2, 7.8 Hz, 4H),4.07 (t, J = 8.2 thiazole-5-carboxamide Hz, 1H), 4.02-3.91 (m, 2H), 3.87(dd, J = 14.7, 7.5 Hz, 1H), 3.74- 3.59 (m, 1H), 3.39 (t, J = 6.5 Hz,2H), 2.31 (dt, J = 15.2, 7.1 Hz, 1H), 2.19 (dq, J = 13.2, 6.6 Hz, 3H),1.73 (td, J = 13.0, 6.4 Hz, 1H), 1.64 (dd, J = 14.5, 7.3 Hz, 2H), 1.01(d, J = 6.5 Hz, 6H). 156 2-{[2-hydroxy-2-(3- ¹H NMR (400 MHz, DMSO-(ESI(+)) methoxyphenyl)ethyl](3- d₆/D₂O) δ ppm 9.03 (s, 1 H), 7.74 m/e488 methoxypropanoyl)amino}- (s, 1 H), 7.66 (s, 1 H), 7.63 (s, 1 H),(M + H)+ N-[3-(1H-imidazol-1- 7.29-7.34 (m, 1 H), 6.89-6.96yl)propyl]-1,3-thiazole-5- (m, 3 H), 5.86-5.90 (m, 1 H), 4.23carboxamide (t, J = 6.71 Hz, 2 H), 3.53-3.66 (m, 4 H), 3.22 (d, J = 2.44Hz, 2 H), 3.20 (s, 3 H), 2.57-2.62 (m, 2 H), 2.02-2.06 (m, 2 H),1.01-1.14 (m, 3 H). 157 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, DMSO-(ESI(+)) yl)propyl]-2-{(3- d₆/D₂O) δ ppm 9.04 (s, 1 H), 8.55- m/e 444methoxypropanoyl)[2- 8.57 (m, 2 H), 8.50 (d, J = 2.14 Hz, (M + H)+(pyrazin-2-yl)ethyl]amino}- 1 H), 8.03 (s, 1 H), 7.75 (t, J = 1.681,3-thiazole-5-carboxamide Hz, 1 H), 7.62-7.65 (m, 1 H), 4.55- 4.59 (m,2 H), 4.25 (t, J = 6.87 Hz, 3 H), 3.65 (t, J = 5.95 Hz, 2 H), 3.24-3.28(m, 7 H), 2.92 (t, J = 6.10 Hz, 2 H), 2.06-2.11 (m, 2 H). 158 2-{[1-(3-¹H NMR (400 MHz, DMSO- (ESI(+)) hydroxyphenyl)propan-2- d₆/D₂O) δ ppm9.02 (s, 1 H), 7.74 m/e 472 yl](3- (t, y = 1.83 Hz, 1 H), 7.63 (s, 2 H),(M + H)+ methoxypropanoyl)amino}- 7.34 (t, J = 7.63 Hz, 1 H), 7.14 (s, 1N-[3-(1H-imidazol-1- H), 6.94-6.98 (m, 1 H), 6.59-yl)propyl]-1,3-thiazole-5- 6.63 (m, 1 H), 4.22 (t, J = 6.87 Hz,carboxamide 2 H), 3.66 (t, J = 6.10 Hz, 3 H), 3.29 (s, 3 H), 3.17-3.24(m, 4 H), 2.80 (t, J = 5.95 Hz, 3 H), 2.00- 2.08 (m, 2 H), 1.15 (d, J =6.41 Hz, 3 H). 173 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, CDCl₃) δ 9.10(ESI(+)) yl)propyl]-2-[(3- (s, 1H), 7.98 (s, 1H), 7.38 (d, J = m/e 434methylbutyl)(tetrahydrofuran- 4.8 Hz, 2H), 6.83 (dd, J = 5.1, 2.6 (M +H)+ 2-ylacetyl)amino]-1,3- Hz, 1H), 4.42 (dd, J = 12.9, 6.7 Hz,thiazole-5-carboxamide 1H), 4.34 (t, J = 6.5 Hz, 2H), 4.20 (t, J = 8.3Hz, 2H), 3.92 (dd, J = 15.0, 6.9 Hz, 1H), 3.80 (dd, J = 15.1, 6.9 Hz,1H), 3.51 (ddd, J = 5.9, 4.6, 2.9 Hz, 2H), 3.04-2.96 (m, 2H), 2.78 (dd,J = 15.9, 5.4 Hz, 2H), 2.25 (dt, J = 15.8, 6.1 Hz, 3H), 1.97 (dt, J =13.9, 6.9 Hz, 2H), 1.79-1.69 (m, 1H), 1.67- 1.52 (m, 3H), 0.99 (d, J =6.5 Hz, 6H). 174 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, CDCl₃) δ 9.15(ESI(+)) yl)propyl]-2-[(3- (s, 1H), 8.00 (s, 1H), 7.37 (d, J = m/e 434methylbutyl)(tetrahydrofuran- 9.6 Hz, 2H), 6.81 (dd, J = 7.5, 3.3 (M +H)+ 3-ylacetyl)amino]-1,3- Hz, 1H), 4.34 (t, J = 6.5 Hz, 2H),thiazole-5-carboxamide 4.15 (dd, J = 9.7, 6.7 Hz, 2H), 4.04 (dd, J =8.7, 6.9 Hz, 1H), 3.94 (td, J = 8.3, 5.1 Hz, 1H), 3.81 (dd, J = 15.9,7.6 Hz, 1H), 3.51 (dt, J = 10.0, 5.1 Hz, 3H), 2.84 (dt, J = 10.4, 4.2Hz, 1H), 2.79-2.66 (m, 2H), 2.36-2.18 (m, 3H), 1.72 (dt, J = 13.2, 6.6Hz, 1H), 1.66-1.55 (m, 3H), 1.05-0.89 (m, 6H). 175 N-[3-(1H-imidazol-1-¹H NMR (400 MHz, CDCl₃) δ 9.21- (ESI(+)) yl)propyl]-2-[(2- 9.10 (m, 1H),7.99 (s, 1H), 7.42- m/e 396 methoxyethyl)(3- 7.33 (m, 2H), 7.04-6.85 (m,1H), (M + H)+ methoxypropanoyl)amino]- 4.40 (t, J = 4.9 Hz, 2H), 4.34(dd, J = 1,3-thiazole-5-carboxamide 9.2, 3.5 Hz, 2H), 3.79 (t, J = 6.2Hz, 2H), 3.68 (t, J = 4.9 Hz, 2H), 3.53-3.46 (m, 2H), 3.39 (s, 3H), 3.30(s, 3H), 3.09 (t, J = 6.2 Hz, 2H), 2.26-2.21 (m, 2H). 176N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, CDCl₃) δ 9.26- (ESI(+))yl)propyl]-2-[(3- 9.13 (m, 1H), 8.05-7.97 (m, m/e 410methoxypropanoyl)(3- 1H), 7.36 (d, J = 8.6 Hz, 2H), 7.04- (M + H)+methoxypropyl)amino]-1,3- 6.87 (m, 1H), 4.40-4.32 (m,thiazole-5-carboxamide 2H), 4.32-4.23 (m, 2H), 3.81 (t, J = 6.1 Hz, 2H),3.50 (d, J = 5.5 Hz, 2H), 3.44 (t, J = 5.6 Hz, 2H), 3.39 (s, 3H), 3.34(s, 3H), 2.98 (t, J = 6.1 Hz, 2H), 2.26-2.20 (m, 2H), 2.08-1.99 (m, 2H).177 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, CDCl₃) δ 9.17 (ESI(+))yl)propyl]-2-[(3- (s, 1H), 8.00 (s, 1H), 7.37 (dd, J = m/e 436methoxypropanoyl)(tetrahydro- 8.1, 3.9 Hz, 2H), 6.88-6.77 (m, (M + H)+2H-pyran-2- 1H), 4.46-4.36 (m, 1H), 4.37- ylmethyl)amino]-1,3- 4.30 (m,2H), 4.03-3.84 (m, 2H), thiazole-5-carboxamide 3.84-3.73 (m, 2H),3.74-3.61 (m, 2H), 3.55-3.46 (m, 2H), 3.39 (s, 3H), 3.33-3.19 (m, 3H),2.99 (dt, J = 16.8, 6.8 Hz, 1H), 2.28- 2.21 (m, 2H), 1.89-1.85 (m, 1H),1.73 (ddd, J = 3.0, 1.3, 0.6 Hz, 1H), 1.52-1.48 (m, 2H), 1.23- 1.13 (m,2H). 178 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, CDCl₃) δ 9.16 (ESI(+))yl)propyl]-2-[(3- (d, J = 4.8 Hz, 1H), 8.00 (d, J = m/e 422methoxypropanoyl)(tetrahydro- 4.2 Hz, 1H), 7.36 (d, J = 7.9 Hz, (M + H)+furan-2-ylmethyl)amino]- 2H), 6.89-6.78 (m, 1H), 4.54 (dd,1,3-thiazole-5-carboxamide J = 14.5, 1.6 Hz, 1H), 4.37-4.30 (m, 2H),4.30-4.23 (m, 1H), 4.10- 3.95 (m, 1H), 3.87 (dd, J = 14.7, 6.5 Hz, 1H),3.82-3.76 (m, 2H), 3.71 (dd, J = 8.2, 6.6 Hz, 1H), 3.55- 3.45 (m, 2H),3.39 (s, 3H), 3.26- 3.12 (m, 1H), 3.03 (dt, J = 16.7, 6.8 Hz, 1H),2.24-2.20 (m, 2H), 1.93 (d, J = 7.2 Hz, 2H), 1.66- 1.50 (m, 2H). 179N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, CDCl₃) δ 9.25- (ESI(+))yl)propyl]-2-{(3- 9.09 (m, 1H), 8.07-7.96 (m, m/e 424methoxypropanoyl)[2- 1H), 7.35 (d, J = 11.4 Hz, 2H), (M + H)+ (propan-2-6.98-6.78 (m, 1H), 4.38 (t, J = yloxy)ethyl]amino}-1,3- 4.9 Hz, 2H),4.36-4.30 (m, 2H), thiazole-5-carboxamide 3.79 (dd, J = 8.1, 4.5 Hz,2H), 3.75- 3.68 (m, 3H), 3.49 (dd, J = 10.9, 4.8 Hz, 2H), 3.38 (s, 3H),3.27 (dd, J = 7.0, 3.4 Hz, 1H), 3.13 (dd, J = 8.1, 4.4 Hz, 2H),2.24-2.20 (m, 2H), 1.06 (d, J = 6.1 Hz, 6H). 180 2-{[2-(1,3-dioxolan-2-¹H NMR (400 MHz, methanol-d₄) (ESI(+)) yl)ethyl](3- δ 8.98 (s, 1H),8.59-8.49 (m, 1H), m/e 438 methoxypropanoyl)amino}- 8.02 (s, 1H), 7.71(d, J = 1.5 Hz, (M + H)+ N-[3-(1H-imidazol-1- 1H), 7.57 (s, 1H), 4.95(t, J = 4.3 yl)propyl]-1,3-thiazole-5- Hz, 1H), 4.37 (dd, J = 12.7, 5.0Hz, carboxamide 2H), 4.34-4.29 (m, 2H), 3.99- 3.91 (m, 2H), 3.85 (dd, J= 8.8, 5.1 Hz, 2H), 3.79 (t, J = 6.0 Hz, 2H), 3.43-3.37 (m, 2H), 3.36(s, 3H), 3.03 (t, J = 6.0 Hz, 2H), 2.26- 2.17 (m, 2H), 2.17-2.11 (m,2H). 181 2-[(l,4-dioxan-2- (ESI(+)) ylmethyl)(3- m/e 438methoxypropanoyl)amino]- (M + H)+ N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5- carboxamide 182 2-{[3-(4- ¹H NMR (400 MHz,methanol-d₄) (ESI(+)) fluorophenyl)propanoyl](2- δ 8.96 (s, 1H), 7.99(s, 1H), 7.70 (t, m/e 55460 methoxyethyl)amino}-N-[3- J = 1.7 Hz, 1H),7.57 (t, J = 1.6 (M + H)+ (1H-imidazol-1-yl)propyl]- Hz, 1H), 7.27 (dd,J = 8.6, 5.5 Hz, 1,3-thiazole-5-carboxamide 2H), 6.99 (t, J = 8.8 Hz,2H), 4.41 (t, J = 5.1 Hz, 2H), 4.33 (t, J = 6.9 Hz, 2H), 3.66 (t, J =5.0 Hz, 2H), 3.40 (t, J = 6.4 Hz, 2H), 3.26 (s, 3H), 3.17 (t, J = 7.3Hz, 2H), 3.01 (t, J = 7.2 Hz, 2H), 2.24-2.09 (m, 2H). 183N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))yl)propyl]-2-{(2- δ 8.98 (s, 1H), 8.84 (s, 1H), 8.70 m/e 443methoxyethyl)[3-(pyridin-3- (d, J = 5.5 Hz, 1H), 8.59 (d, J = (M + H)+yl)propanoyl]amino}-1,3- 8.2 Hz, 1H), 8.01 (dd, J = 8.1, 5.7thiazole-5-carboxamide Hz, 1H), 7.99 (s, 1H), 7.70 (t, J = 1.7 Hz, 1H),7.57 (t, , J = 1.7 Hz, 1H), 4.45 (t, J = 5.0 Hz, 2H), 4.32 (t, J = 6.9Hz, 2H), 3.69 (t, J = 4.9 Hz, 2H), 3.40 (dt, J = 9.9, 6.9 Hz, 4H), 3.27(s, 3H), 2.18 (m, 2H). 184 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz,methanol-d₄) (ESI(+)) yl)propyl]-2-[(2- δ 8.97 (s, 1H), 8.81 (d, J = 9.1Hz, m/e 429 methoxyethyl)(pyridin-3- 2H), 8.52 (d, J = 8.1 Hz, 1H), 8.06(M + H)+ ylacetyl)amino]-1,3- (dd, J = 7.9, 5.9 Hz, 1H), 8.04 (s,thiazole-5-carboxamide 1H), 7.70 (t, J = 1.7 Hz, 1H), 7.56 (t, J = 1.7Hz, 1H), 4.61 (t, J = 5.0 Hz, 2H), 4.58 (s, 2H), 4.32 (t, J = 6.9 Hz,2H), 3.80 (t, J = 4.9 Hz, 2H), 3.39 (t, J = 6.4 Hz, 2H), 3.38 (s, 3H),2.18 (m, 2H). 185 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, methanol-d₄)(ESI(+)) yl)propyl]-2-[(2- δ 8.98 (s, 1H), 8.04 (s, 1H), 7.92- m/e 478methoxyethyl)(naphthalen- 7.79 (m, 0033H), 7.74 (d, J = 15.9 (M + H)+2-ylacetyl)amino]-1,3- Hz, 2H), 7.59 (s, 1H), 7.51 (dd, J =thiazole-5-carboxamide 6.8, 2.8 Hz, 2H), 7.42 (dd, J = 8.5, 1.7 Hz, 1H),4.57 (t, J = 5.1 Hz, 2H), 4.44 (s, 2H), 4.35 (t, J = 6.8 Hz, 2H), 3.78(t, J = 5.0 Hz, 2H), 3.42 (t, J = 6.2 Hz, 2H), 3.40 (s, 3H), 2.29-2.11(m, 2H). 186 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))yl)propyl]-2-{(2- δ 8.95 (s, 1H), 8.03 (t, J = 1.3 Hz, m/e 520methoxyethyl)[(4- 1H), 7.70 (s, 1H), 7.58 (s, 1H), (M + H)+phenoxyphenyl)acetyl]amino}- 7.40-7.33 (m, 2H), 7.27 (d, J =1,3-thiazole-5- 8.5 Hz, 2H), 7.12 (dd, J = 11.3, 3.9 carboxamide Hz,2H), 7.03-6.95 (m, 4H), 4.52 (t, J = 5.1 Hz, 2H), 4.35 (t, J = 6.9 Hz,2H), 4.24 (s, 2 H), 3.76 (t, J = 5.1 Hz, 2H), 3.43 (t, J = 6.5 Hz, 2H),3.38 (s, 3H), 2.34-2.12 (m, 2H). 187 2-{[(4- ¹H NMR (400 MHz,methanol-d₄) (ESI(+)) cyanophenyl)acetyl](2- δ ppm 8.94 (s, 1 H), 8.01(s, 1H), m/e 453 methoxyethyl)amino}-N-[3- 7.70 (m, 3 H), 7.55 (s, 1 H),7.44 (M + H)+ (1H-imidazol-1-yl)propyl]- (d, J = 8.1 Hz, 2H), 4.53 (t, J= 4.9 1,3-thiazole-5-carboxamide Hz, 2H), 4.35 (s, 2H), 4.32 (t, J = 6.9Hz, 2H), 3.75 (t, J = 4.9 Hz, 2H), 3.39 (t, J = 6.5 Hz, 2H), 3.36 (s,3H), 2.19 (m, 2H). 188 2-{[(4- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))aminophenyl)acety1](2- δ 9.02 (s, 1H), 8.07 (s, 1H), 7.74 (s, m/e 443methoxyethyl)amino}-N-[3- 1H), 7.59 (s, 1H), 7.47 (d, J = 8.4 (M + H)+(1H-imidazol-1-yl)propyl]- Hz, 2H), 7.40 (d, J = 8.4 Hz, 2H),1,3-thiazole-5-carboxamide 4.57 (t, J = 4.9 Hz, 2H), 4.40- 4.28 (m, 4H),3.79 (t, J = 5.0 Hz, 2H), 3.42 (t, J = 6.5 Hz, 2H), 3.39 (s, 3H), 2.21(m, 2H). 189 2-[{2-[di(prop-2-en-1- ¹H NMR (400 MHz, DMSO- (ESI(+))yl)amino]ethyl}(3- d₆/D₂O) δ ppm 8.98 (s, 1 H), 8.05 m/e 461methoxypropanoyl)amino]- (s, 1 H), 7.70 (s, 1 H), 7.59 (s, 1 H), (M +H)+ N-[3-(1H-imidazol-1- 5.89-6.01 (m, 2 H), 5.49-5.59yl)propyl]-1,3-thiazole-5- (m, 4 H), 4.51 (t, 2 H), 4.27 (t, J =carboxamide 7.02 Hz, 2 H), 3.77 (d, J = 7.02 Hz, 4 H), 3.72 (t, J = 6.26Hz, 2 H), 3.31-3.37 (m, 3 H), 3.29 (s, 4 H), 2.98 (t, J = 6.26 Hz, 2H).190 2-{[3- ¹H NMR (400 MHz, DMSO- (ESI(+)) (diethylamino)propyl](3-d₆/D₂O) δ ppm 8.96 (s, 1 H), 8.04 m/e 451 methoxypropanoyl)amino}- (s, 1H), 7.69 (s, 1 H), 7.57 (s, 1 H), (M + H)+ N-[3-(1H-imidazol-1-4.21-4.30 (m, 4 H), 3.74 (t, J = yl)propyl]-1,3-thiazole-5- 6.10 Hz, 2H), 3.31 (s, 2 H), 3.29 carboxamide (s, 3 H), 3.12-3.20 (m, 6 H), 2.98(t, J = 6.10 Hz, 2 H), 2.07-2.15 (m, 4H), 1.23 (t, J = 7.17 Hz, 6 H).191 2-{[2-(diethylamino)ethyl](3- ¹H NMR (400 MHz, DMSO- (ESI(+))methoxypropanoyl)amino}- d₆/D₂O) δ ppm 8.97 (s, 1 H), 8.07 m/e 437N-[3-(1H-imidazol-1- (s, 1 H), 7.69 (s, 1 H), 7.58 (s, 1 H), (M + H)+yl)propyl]-1,3-thiazole-5- 4.52 (t, 2 H), 4.27 (t, J = 7.02 Hz, 2carboxamide H), 3.74 (t, J = 6.10 Hz, 2 H), 3.44 (t, 2 H), 3.30 (s, 4H), 3.29-3.29 (m, 3 H), 3.27 (s, 2 H), 3.01 (t, J = 6.10 Hz, 2 H),2.07-2.16 (m, 2 H), 1.29 (t, J = 7.32 Hz, 6 H). 192 N-[3-(1H-imidazol-1-¹H NMR (400 MHz, DMSO- (ESI(+)) yl)propyl]-2-{(3- d₆/D₂O) δ ppm 8.97 (s,1 H), 8.04 m/e 449 methoxypropanoyl)[3- (s, 1 H), 7.69 (s, 1 H), 7.57(s, 1 H), (M + H)+ (pyrrolidin-1- 4.21-4.31 (m, 4 H), 3.74 (t, J =yl)propyl]amino}-1,3- 5.95 Hz, 2 H), 3.29-3.3 l (m, 6thiazole-5-carboxamide H), 3.22-3.27 (m, 5 H), 2.98 (t, J = 6.10 Hz, 2H), 2.07-2.16 (m, 4 H), 1.94-2.03 (m, 4 H). 193 2-{[(1-ethyl-5- ¹H NMR(400 MHz, DMSO- (ESI(+)) oxopyrrolidin-3- d₆/D₂O) δ ppm 8.97 (s, 1 H),8.02 m/e 463 yl)methyl](3- (s, 1 H), 7.69 (s, 1 H), 7.57 (s, 1 H), (M +H)+ methoxypropanoyl)amino}- 4.24-4.33 (m, 4 H), 3.72 (t, J =N-[3-(1H-imidazol-1- 6.10 Hz, 2 H), 3.41 (dd, J = 9.77,yl)propyl]-1,3-thiazole-5- 7.63 Hz, 1 H), 3.29-3.31 (m, 2 H),carboxamide 3.27 (s, 4 H), 3.14-3.21 (m, 3 H), 2.96 (t, J = 5.95 Hz, 2H), 2.35 (dd, J = 16.63, 8.70 Hz, 1 H), 2.08- 2.15 (m, 3 H), 1.00-1.04(m, 3 H). 194 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, DMSO- (ESI(+))yl)propyl]-2-{(3- d₆/D₂O) δ ppm 8.94 (s, 1 H), 8.01 m/e 435methoxypropanoyl)[(5- (s, 1 H), 7.68 (s, 1 H), 7.56 (s, 1 H), (M + H)+oxopyrrolidin-2- 4.21-4.31 (m, 4 H), 3.72 (t, J = yl)methyl]amino}-1,3-6.26 Hz, 2 H), 3.29-3.31 (m, 2 thiazole-5-carboxamide H), 3.28 (s, 3 H),2.89-3.04 (m, 3 H), 2.24-2.31 (m, 1 H), 2.07- 2.19 (m, 4 H), 1.77-1.84(m, 1 H). 195 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, DMSO- (ESI(+))yl)propyl]-2-{(3- d₆/D₂O) δ ppm 8.97 (s, 1 H), 8.02 m/e 463methoxypropanoyl)[3-oxo- (s, 1 H), 7.69 (s, 1 H), 7.57 (s, 1 H), (M +H)+ 3-(pyrrolidin-1- 4.39-4.43 (m, 2 H), 4.27 (t, J =yl)propyl]amino}-1,3- 7.02 Hz, 2 H), 3.71 (t, J = 6.10thiazole-5-carboxamide Hz, 2 H), 3.29-3.43 (m, 8 H), 3.03 (t, J = 6.26Hz, 2 H), 2.71-2.76 (m, 2 H), 2.08-2.15 (m, 2 H), 1.73- 1.89 (m, 4 H).196 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, DMSO- (ESI(+))yl)propyl]-2-{(3- d₆/D₂O) δ ppm 8.97 (s, 1 H), 7.95 m/e 463methoxypropanoyl)[2-oxo- (s, 1 H), 7.69 (s, 1 H), 7.57 (s, 1 H), (M +H)+ 2-(piperidin-1- 5.13 (s, 2 H), 4.27 (t, J = 7.02 Hz, 2yl)ethyl]amino}-1,3- H), 3.68 (t, J = 6.26 Hz, 2 H), 3.42-thiazole-5-carboxamide 3.54 (m, 4 H), 3.29-3.31 (m, 2 H), 3.27-3.27 (m,3 H), 2.80 (t, J = 6.26 Hz, 2 H), 2.07-2.15 (m, 2 H), 1.47-1.68 (m, 6H). 197 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, DMSO- (ESI(+))yl)propyl]-2-{(3- d₆/D₂O) δ ppm 8.98 (s, 1 H), 8.03 m/e 463methoxypropanoyl)[3-(2- (s, 1 H), 7.67-7.72 (m, 1 H), 7.57 (M + H)+oxopyrrolidin-1- (s, 1 H), 4.27 (t, J = 7.02 Hz, 2 H),yl)propyl]amino}-1,3- 4.15-4.19 (m, 2 H), 3.72 (t, J =thiazole-5-carboxamide 6.10 Hz, 2 H), 3.38 (t, J = 7.02 Hz, 2 H), 3.31(s, 1 H), 3.28 (s, 5 H), 3.26 (s, 1 H), 2.95 (t, J = 6.10 Hz, 2 H), 2.24(t, J = 8.09 Hz, 2 H), 2.07-2.15 (m, 2 H), 1.88-2.00 (m, 4 H). 198N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, DMSO- (ESI(+)) yl)propyl]-2-{(3-d₆/D₂O) δ ppm 8.97 (s, 1 H), 8.03 m/e 451 methoxypropanoyl)[2-(2- (s, 1H), 7.69 (s, 1 H), 7.57 (s, 1 H), (M + H)+ oxo-1,3-oxazolidin-3- 4.39(t, J = 6.26 Hz, 2 H), 4.27 (t, J = yl)ethyl]amino}-1,3- 7.02 Hz, 2 H),4.16-4.20 (m, 2 thiazole-5-carboxamide H), 3.73 (t, J = 6.10 Hz, 2 H),3.57- 3.62 (m, 2 H), 3.53 (t, J = 6.26 Hz, 2 H), 3.28-3.32 (m, 5 H),2.98 (t, J = 6.26 Hz, 2 H), 2.08-2.15 (m, 2 H). 199 N-[3-(1H-imidazol-1-¹H NMR (400 MHz, DMSO- (ESI(+)) yl)propyl]-2-[(3- d₆/D₂O) δ ppm 8.97 (s,1 H), 8.02 m/e 451 methoxypropanoyl){2-[(2- (s, 1 H), 7.66-7.71 (m, 1H), 7.57- (M + H)+ methylpropanoyl)amino]eth- 7.58 (m, 1 H), 4.26 (q, J= 6.92 yl}amino]-1,3-thiazole-5- Hz, 4 H), 3.71 (t, J = 6.10 Hz, 2 H),carboxamide 3.43 (t, J = 6.41 Hz, 2 H), 3.29- 3.32 (m, 2 H), 3.28 (s, 3H), 3.00 (t, J = 6.26 Hz, 2 H), 2.27-2.35 (m, 1 H), 2.08-2.15 (m, 2 H),0.98 (d, J = 7.02 Hz, 6 H). 200 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz,DMSO- (ESI(+)) yl)propyl]-2-{(3- d₆/D₂O) δ ppm 8.97 (s, 1 H), 8.02 m/e423 methoxypropanoyl)[3- (s, 1 H), 7.69 (s, 1 H), 7.57 (s, 1 H), (M +H)+ (methylamino)-3- 4.37-4.41 (m, 2 H), 4.27 (t, J =oxopropyl]amino}-1,3- 7.02 Hz, 2 H), 3.71 (t, J = 6.10thiazole-5-carboxamide Hz, 2 H), 3.31 (s, 2 H), 3.28 (s, 3 H), 3.01 (t,J = 6.26 Hz, 2 H), 2.58 (s, 3 H), 2.07-2.15 (m, 2 H). 201 2-{[3- ¹H NMR(400 MHz, DMSO- (ESI(+)) (acetylamino)propyl](3- d₆/D₂O) δ ppm 8.98 (s,1 H), 8.02 m/e 437 methoxypropanoyl)amino}- (s, 1 H), 7.68-7.70 (m, 1H), 7.57 (M + H)+ N-[3-(1H-imidazol-1- (s, 1 H), 4.27 (t, J = 7.02 Hz, 2H), yl)propyl]-1,3-thiazole-5- 4.17-4.22 (m, 2 H), 3.72 (t, J =carboxamide 6.10 Hz, 2 H), 3.31 (s, 2 H), 3.28 (s, 3 H), 3.13 (t, J =6.87 Hz, 2 H), 2.94 (t, J = 6.10 Hz, 2 H), 2.08- 2.15 (m, 2 H),1.85-1.90 (m, 2 H), 1.84 (s, 3 H). 202 N-[3-(1H-imidazol-1- ¹H NMR (400MHz, DMSO- (ESI(+)) yl)propyl]-2-{(3- d₆/D₂O) δ ppm 8.96-8.98 (m, 1 m/e449 methoxypropanoyl)[2-oxo- H), 8.02 (s, 1 H), 7.68-7.70 (m, 1 (M + H)+2-(pyrrolidin-1- H), 7.58 (s, 1 H), 4.25-4.32 (m, 4 yl)ethyl]amino}-1,3-H), 3.72 (t, J = 5.95 Hz, 2 H), 3.40 thiazole-5-carboxamide (dd, J =10.07, 7.63 Hz, 1 H), 3.29- 3.31 (m, 2 H), 3.28-3.29 (m, 3 H), 3.15 (dd,J = 10.07, 5.49 Hz, 1 H), 2.95 (t, J = 6.10 Hz, 2 H), 2.85- 2.92 (m, 1H), 2.71 (s, 3 H), 2.34 (dd, J = 16.63, 8.70 Hz, 1 H), 2.08- 2.15 (m, 3H). 205 2-{[(5-chloropyridin-2- ¹H NMR (500 MHz, methanol-d₄) (ESI(+))yl)methyl](tetrahydro-2H- δ 8.97 (s, 1H), 8.45 (d, J = 2.3 Hz, m/e 489pyran-4-ylcarbonyl)amino}- 1H), 7.91 (s, 1H), 7.81 (dd, J = 8.4, (M +H)+ N-[3-(1H-imidazol-1- 2.4 Hz, 1H), 7.70 (s, 1H), 7.56 (s,yl)propyl]-1,3-thiazole-5- 1H), 7.42 (d, J = 8.4 Hz, 1H), 5.66carboxamide (s, 2H), 4.32 (t, J = 6.9 Hz, 2H), 3.96 (dd, J = 11.6, 2.0Hz, 2H), 3.44 (t, J = 11.2 Hz, 2H), 3.38 (t, J = 6.4 Hz, 2H), 3.26 (dt,J = 7.0, 5.2 Hz, 1H), 2.18 (p, J = 6.7 Hz, 2H), 1.90 (qd, J = 12.3, 4.4Hz, 2H), 1.73 (d, J = 13.1 Hz, 2H). 206 2-{[(5-chloropyridin-2- ¹H NMR(500 MHz, methanol-d₄) (ESI(+)) yl)methyl](tetrahydrofuran- δ 8.97 (s,1H), 8.45 (d, J = 2.4 Hz, m/e 475 3-ylcarbonyl)amino}-N-[3- 1H),7.95-7.76 (m, 2H), 7.70 (t, J = (M + H)+ (1H-imidazol-1-yl)propyl]- 1.6Hz, 1H), 7.56 (t, J = 1.6 Hz, 1,3-thiazole-5-carboxamide 1H), 7.42 (d, J= 8.5 Hz, 1H), 5.66 (s, 2H), 4.32 (t, J = 6.9 Hz, 2H), 3.97 (dq, J =14.5, 6.0 Hz, 3H), 3.80 (dt, J = 14.3, 7.3 Hz, 2H), 3.38 (t, J = 6.4 Hz,2H), 2.19 (tt, J = 13.2, 6.8 Hz, 4H). 207 2-{[2-(5-chloropyridin-2- ¹HNMR (400 MHz, methanol-d₄) (ESI(+)) yl)ethyl](3- δ 9.00 (s, 1H), 8.52(d, J = 2.5 Hz, m/e 477 methoxypropanoyl)amino}- 1H), 8.01 (s, 1H), 7.81(dd, J = 8.4, (M + H)+ N-[3-(1H-imidazol-1- 2.5 Hz, 1H), 7.72 (t, J =1.6 Hz, yl)propyl]-1,3-thiazole-5- 1H), 7.58 (t, J = 1.6 Hz, 1H), 7.32carboxamide (d, J = 8.4 Hz, 1H), 4.69-4.54 (m, 2H), 4.34 (t, J = 6.8 Hz,2H), 3.73 (t, J = 5.9 Hz, 2H), 3.40 (t, J = 6.4 Hz, 2H), 3.34 (s, 3H),3.27 (d, J = 7.3 Hz, 2H), 2.90 (t, J = 5.9 Hz, 2H), 2.27-2.08 (m, 2H).208 2-{[2-(5-chloropyridin-2- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))yl)ethyl](tetrahydrofuran-3- δ 9.00 (s, 1H), 8.51 (d, J = 2.5 Hz, m/e489 ylcarbonyl)amino}-N-[3- 1H), 8.03 (s, 1H), 7.79 (dd, J = 8.3, (M +H)+ (1H-imidazol-1-yl)propyl]- 2.5 Hz, 1H), 7.72 (t, J = 1.6 Hz,1,3-thiazole-5-carboxamide 1H), 7.58 (t, J = 1.5 Hz, 1H), 7.32 (d, J =8.4 Hz, 1H), 4.64 (dd, J = 8.2, 6.1 Hz, 2H), 4.34 (t, J = 6.8 Hz, 2H),4.01-3.94 (m, 1H), 3.91 (dd, J = 8.5, 5.9 Hz, 2H), 3.86- 3.79 (m, 1H),3.71-3.56 (m, 1H), 3.40 (t, J = 6.5 Hz, 2H), 3.28 (d, J = 7.1 Hz, 2H),2.27-2.18 (m, 2H), 2.17-1.98 (m, 2H). 209 2-{[2-(5-chloropyridin-2- ¹HNMR (400 MHz, methanol-d₄) (ESI(+)) yl)ethyl][(2- δ 8.99 (s, 1H), 8.54(d, J = 2.4 Hz, m/e 493 methoxyethyl)carbamoyl]a 1H), 8.01-7.77 (m, 2H),7.71 (t, J = (M + H)+ mino}-N-[3-(1H-imidazol- 1.6 Hz, 1H), 7.58 (t, J =1.5 Hz, 1-yl)propyl]-1,3-thiazole-5- 1H), 7.35 (d, J = 8.4 Hz, 1H), 4.46carboxamide (t, J = 7.1 Hz, 2H), 4.33 (t, J = 6.9 Hz, 2H), 3.51 (dd, J =8.2, 3.0 Hz, 2H), 3.45 (t, J = 5.1 Hz, 2H), 3.40 (t, J = 6.7 Hz, 2H),3.38 (s, 3H), 3.24 (t, J = 7.1 Hz, 2H), 2.18 (p, J = 6.7 Hz, 2H). 2102-([2-(5-chloropyridin-2- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))yl)ethyl]{[2-(propan-2- δ 8.99 (s, 1H), 8.54 (d, J = 2.5 Hz, m/e 521yloxy)ethyl]carbamoyl}ami- 1H), 7.89 (s, 1H), 7.80 (dd, J = 8.4, (M +H)+ no)-N-[3-(1H-imidazol-1- 2.5 Hz, 1H), 7.71 (s, 1H), 7.58 (d, J =yl)propyl]-1,3-thiazole-5- 1.5 Hz, 1H), 7.34 (d, J = 8.4 Hz, carboxamide1H), 4.46 (t, J = 7.1 Hz, 2H), 4.33 (t, J = 6.8 Hz, 2H), 3.65 (dt, J =12.2, 6.1 Hz, 1H), 3.56 (t, J = 5.7 Hz, 2H), 3.43 (t, J = 5.6 Hz, 2H),3.38 (t, J = 6.4 Hz, 2H), 3.22 (dt, J = 7.8, 4.0 Hz, 2H), 2.18 (p, J =6.7 Hz, 2H), 1.16 (d, J = 6.1 Hz, 6H). 211 2-[(1,3-benzodioxol-5- ¹H NMR(400 MHz, methanol-d₄) (ESI(+)) ylacetyl)(2- δ 8.01 (s, 1H), 7.71 (s,1H), 7.19 (s, m/e 472 methoxyethyl)amino]-N-[3- 1H), 6.98 (s, 1H),6.87-6.69 (m, (M + H)+ (1H-imidazol-1-yl)propyl]- 3H), 5.95 (s, 2H),4.49 (t, J = 5.0 1,3-thiazole-5-carboxamide Hz, 2H), 4.15 (s, 3H), 4.12(t, J = 7.0 Hz, 2H), 3.73 (t, J = 5.1 Hz, 2H), 3.40-3.35 (m, 5H), 2.17-1.88 (m, 2H). 213 N-[3-(1H-imidazol-1- ¹H NMR (400 MHz, DMSO-d₆) δ(ESI(+)) yl)propyl]-2-[(2- 8.55-8.31 (m, 1H), 8.09 (s, 1H), m/e 429methoxyethyl)(pyridin-2- 7.79 (td, J = 7.7, 1.8 Hz, 1H), 7.64 (M + H)+ylacetyl)amino]-1,3- (s, 1H), 7.64 (s, 1H), 7.37 (d, J =thiazole-5-carboxamide 7.8 Hz, 1H), 7.31 (dd, J = 7.5, 4.9 Hz, 1H), 7.19(s, 1H), 6.88 (s, 1H), 4.45 (t, J = 5.2 Hz, 2H), 4.00 (t, J = 6.9 Hz,2H), 3.66 (t, J = 5.3 Hz, 2H), 3.26 (s, 3H), 3.23-3.11 (m, 2H),2.16-1.83 (m, 2H).

Example 462-[(4-fluorobenzyl)(propan-2-ylcarbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide

Example 6B (0.072 g, 0.2 mmol) was dissolved in acetonitrile (1 ml) andpyridine (0.1 ml) and treated withbis(2,5-dioxopyrrolidin-1-yl)carbonate (0.064 g, 0.25 mmol). Thereaction mixture was stirred at 50° C. for 3 hours, cooled, and treatedwith Hunig's base (0.105 ml, 0.6 mmol) and propan-2-amine (0.02 ml, 0.23mmol). The reaction mixture was stirred further at 25° C. for 3 hours,concentrated purified by reverse-phase HPLC (as described in Example 6C)to provide the title compound. ¹H NMR (400 MHz, DMSO-d₆) δ 9.12 (s, 1H),8.45 (t, J=5.6 Hz, 1H), 7.90 (s, 1H), 7.82 (d, J=1.5 Hz, 1H), 7.70 (d,J=1.5 Hz, 1H), 7.48 (d, J=7.6 Hz, 1H), 7.22 (dd, J=8.7, 5.7 Hz, 2H),7.16 (t, J=8.9 Hz, 2H), 5.37 (s, 2H), 4.22 (t, J=7.0 Hz, 2H), 3.93-3.87(m, 1H), 3.21 (q, J=6.3 Hz, 2H), 2.04 (t, J=6.8 Hz, 2H), 1.10 (d, J=6.6Hz, 6H); MS (ESI(+)) m/e 444.5 (M+H)+.

The following examples were prepared as described in Example 6B followedby Example 46, substituting the appropriate amines in Example 6B andExample 46. Title compounds were purified by either flash chromatography(silica gel column eluting with a gradient of 0-10% methanol indichloromethane) or reverse-phase HPLC (as described in Example 6C).Accordingly, some examples were isolated as trifluoroacetic acid salts.

EX NAME ¹H NMR DATA MS DATA 63 2-{(4-fluorobenzyl)[(3- ¹H NMR (400 MHz,CDCl₃) δ (ESI(+)) methylbutyl)carbamoyl]amino}- 9.15 (s, 1H), 8.70 (s,1H), 7.83 (s, m/e 473 N-[3-(1H-imidazol-1- 1H), 7.32 (d, J = 20.0 Hz,2H), (M + H)+ yl)propyl]-1,3-thiazole-5- 7.27 (dd, J = 9.4, 4.5 Hz, 2H),carboxamide 7.11 (s, 1H), 7.02 (t, J = 8.6 Hz, 2H), 5.15 (s, 2H), 4.30(t, J = 6.5 Hz, 2H), 3.44-3.38 (m, 4H), 2.26- 2.16 (m, 2H), 1.62 (dt, J= 13.4, 6.8 Hz, 1H), 1.48 (dd, J = 14.6, 7.1 Hz, 2H), 0.92 (t, J = 6.8Hz, 6H). 64 2-{(4-fluorobenzyl)[(2- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+))methylpropyl)carbamoyl]amino}- 9.15 (s, 1H), 8.80 (s, 1H), 7.84 (s, m/e459 N-[3-(1H-imidazol-1- 1H), 7.35 (s, 1H), 7.30 (s, 1H), (M + H)+yl)propyl]-1,3-thiazole-5- 7.27 (d, J = 4.4 Hz, 2H), 7.04 (s,carboxamide 1H), 7.02 (t, J = 8.5 Hz, 2H), 5.16 (s, 2H), 4.30 (t, J =6.5 Hz, 2H), 3.44 (dd, J = 11.6, 6.0 Hz, 2H), 3.22 (t, J = 6.0 Hz, 2H),2.28- 2.17 (m, 2H), 1.85 (dd, J = 13.5, 6.7 Hz, 1H), 0.93 (d, J = 6.6Hz, 6H). 65 N¹-(4-fluorobenzyl)-N¹-(5- ¹H NMR (400 MHz, CDCl₃) δ(ESI(+)) {[3-(1H-imidazol-1- 9.16 (dd, J = 1.6, 1.0 Hz, 1H), m/e 514yl)propyl]carbamoyl}-1,3- 7.79 (s, 1H), 7.34 (d, J = 0.5 Hz, (M + H)+thiazol-2-yl)piperidine-1,3- 1H), 7.33-7.31 (m, 1H), 7.30 (d,dicarboxamide J = 5.4 Hz, 1H), 7.28 (s, 1H), 7.03- 6.97 (m, 3H),6.82-6.75 (m, 1H), 6.48-6.39 (m, 1H), 5.04 (d, J = 9.7 Hz, 2H),4.36-4.30 (m, 2H), 3.69-3.62 (m, 1H), 3.56 (s, 1H), 3.50-3.42 (m, 3H),3.04 (ddd, J = 11.6, 6.9, 2.5 Hz, 1H), 2.49 (d, J = 3.9 Hz, 1H), 2.26-2.21 (m, 2H), 1.42-1.33 (m, 2H), 0.97 (t, J = 7.4 Hz, 2H). 662-{(4-fluorobenzyl)[(3- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))hydroxyazetidin-1- δ 8.98 (s, 1H), 7.85 (s, 1H), 7.70 m/e 459yl)carbonyl]amino}-N-[3- (d, J = 1.6 Hz, 1H), 7.57 (s, 1H), (M + H)+(1H-imidazol-1-yl)propyl]- 7.21 (dd, J = 8.6, 5.3 Hz, 2H),1,3-thiazole-5-carboxamide 7.05 (t, J = 8.7 Hz, 2H), 5.28 (s, 2H), 4.49(ddd, J = 11.2, 5.6, 3.4 Hz, 1H), 4.31 (dd, J = 14.6, 7.2 Hz, 4H), 3.88(dd, J = 9.6, 4.4 Hz, 2H), 3.37 (dd, J = 12.9, 6.5 Hz, 2H), 2.17 (p, J =6.7 Hz, 2H). 67 N-(4-fluorobenzyl)-N-(5- ¹H NMR (400 MHz, CDCl₃) δ(ESI(+)) {[3-(1H-imidazol-1- 9.07 (s, 1H), 7.84 (s, 1H), 7.34 (d, m/e515 yl)propyl]carbamoyl}-1,3- J = 13.9 Hz, 2H), 7.30-7.24 (m, (M + H)+thiazol-2-yl)-1,4-dioxa-7- 2H), 6.99 (t, J = 8.5 Hz, 2H), 6.86azaspiro[4.4]nonane-7- (s, 1H), 5.09 (s, 2H), 4.29 (t, J = carboxamide6.3 Hz, 2H), 3.96 (dd, J = 11.8, 3.4 Hz, 4H), 3.91 (dd, J = 12.4, 5.1Hz, 2H), 3.61 (t, J = 7.2 Hz, 2H), 3.48-3.52 (m, 2H), 2.24- 2.19 (m,2H), 2.04 (t, J = 7.3 Hz, 2H). 68 2-{(4-fluorobenzyl)[(3- ¹H NMR (400MHz, CDCl₃) δ (ESI(+)) methoxypyrrolidin-1- 9.06 (s, 1H), 7.85 (s, 1H),7.34 (s, m/e 487 yl)carbonyl]amino}-N-[3- 1H), 7.31 (s, 1H), 7.29-7.24(m, (M + H)+ (1H-imidazol-1-yl)propyl]- 2H), 7.16 (s, 1H), 6.98 (t, J =8.6 1,3-thiazole-5-carboxamide Hz, 2H), 5.19-5.01 (m, 2H), 4.29 (t, J =6.5 Hz, 2H), 3.94 (s, 1H), 3.56 (dt, J = 12.6, 7.3 Hz, 2H), 3.46 (dd, J= 13.5, 7.7 Hz, 4H), 3.27 (s, 3H), 2.23-2.16 (m, 2H), 2.09-2.03 (m, 1H),1.98-1.81 (m, 1H). 69 2-{(4-fluorobenzyl)[(2- ¹H NMR (400 MHz, CDCl₃) δ(ESI(+)) methoxyethyl)(methyl)carbam- 9.10 (s, 1H), 7.82 (s, 1H), 7.34(d, m/e 475 oyl]amino}-N-[3-(1H- J = 8.9 Hz, 3H), 7.28 (s, 1H), 7.11(M + H)+ imidazol-1-yl)propyl]-1,3- (s, 1H), 6.98 (t, J = 8.6 Hz, 2H),thiazole-5-carboxamide 5.03 (s, 2H), 4.29 (t, J = 6.3 Hz, 2H), 3.49 (s,4H), 3.43 (d, J = 5.4 Hz, 2H), 3.30 (s, 3H), 2.98 (s, 3H), 2.21-2.16 (m,2H). 70 N-(4-fluorobenzyl)-N-(5- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+)){[3-(1H-imidazol-1- 9.16-9.05 (m, 1H), 7.81 (s, 1H), m/e 501yl)propyl]carbamoyl}-1,3- 7.38-7.28 (m, 4H), 7.03-6.95 (M + H)+thiazol-2-yl)-2,6- (m, 2H), 6.96-6.88 (m, 1H), 5.06dimethylmorpholine-4- (s, 2H), 4.30 (dd, J = 8.4, 4.0 Hz, carboxamide2H), 3.65 (d, J = 12.8 Hz, 2H), 3.45 (dd, J = 6.9, 3.2 Hz, 4H), 2.66(dd, J = 12.9, 10.8 Hz, 2H), 2.21-2.17 (m, 2H), 1.12 (d, J = 6.2 Hz,6H). 71 2-{[ethyl(2- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+))methoxyethyl)carbamoyl](4- 9.07 (s, 1H), 7.80 (s, 1H), 7.41- m/e 489fluorobenzyl)amino}-N-[3- 7.28 (m, 4H), 6.98 (t, J = 8.6 Hz, (M + H)+(1H-imidazol-1-yl)propyl]- 3H), 5.04 (s, 2H), 4.29 (d, J = 6.11,3-thiazole-5-carboxamide Hz, 2H), 3.50-3.39 (m, 6H), 3.37 (d, J = 7.0Hz, 2H), 3.29 (s, 3H), 2.20-2.16 (m, 2H), 1.07 (t, J = 7.0 Hz, 3H). 72N-(4-fluorobenzyl)-N-(5- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+)){[3-(1H-imidazol-1- 9.12-9.04 (m, 1H), 7.80 (s, 1H), m/e 501yl)propyl]carbamoyl}-1,3- 7.34 (dt, J = 4.2, 3.7 Hz, 3H), (M + H)+thiazol-2-yl)-2,2- 7.29 (d, J = 0.4 Hz, 1H), 7.03- dimethylmorpholine-4-6.95 (m, 2H), 6.86-6.79 (m, 1H), carboxamide 5.06 (s, 2H), 4.29 (td, J =6.4, 3.2 Hz, 2H), 3.64 (dd, J = 5.9, 3.7 Hz, 2H), 3.48-3.41 (m, 2H),3.39- 3.34 (m, 2H), 3.21 (d, J = 3.6 Hz, 2H), 2.23-2.17 (m, 2H), 1.10(d, J = 4.9 Hz, 6H). 73 N-(4-fluorobenzyl)-N-(5- ¹H NMR (400 MHz, CDCl₃)δ (ESI(+)) {[3-(1H-imidazol-1- 9.14-9.06 (m, 1H), 7.80 (s, 1H), m/e 487yl)propyl]carbamoyl}-1,3- 7.38-7.33 (m, 3H), 7.28 (s, 1H), (M + H)+thiazol-2-yl)-1,4-oxazepane- 7.00 (t, J = 8.6 Hz, 2H), 6.94 (s,4-carboxamide 1H), 5.02 (s, 2H), 4.30 (dd, J = 7.9, 4.8 Hz, 2H),3.66-3.62 (m, 2H), 3.62-3.58 (m, 2H), 3.53 (dd, J = 11.0, 5.9 Hz, 4H),3.48- 3.39 (m, 2H), 2.21-2.17 (m, 2H), 1.85 (dd, J = 10.1, 4.6 Hz, 2H).78 2-{(4-fluorobenzyl)[(2- ¹H NMR (400 MHz, DMSO-d₆) δ (ESI(+))propoxyethyl)carbamoyl]amino}- 9.11 (s, 1H), 8.46 (t, J = 5.7 Hz, m/e489 N-[3-(1H-imidazol-1- 1H), 7.90 (s, 1H), 7.85 (t, J = 5.3 (M + H)⁺yl)propyl]-1,3-thiazole-5- Hz, 1H), 7.81 (t, J = 1.4 Hz, 1H),carboxamide 7.69 (t, J = 1.4 Hz, 1H), 7.23 (dd, J = 8.6, 5.6 Hz, 2H),7.13 (dd, J = 12.3, 5.4 Hz, 2H), 5.33 (s, 2H), 4.22 (t, J = 6.9 Hz, 2H),3.40 (t, J = 5.6 Hz, 2H), 3.32 (dd, J = 10.9, 5.4 Hz, 2H), 3.26 (d, J =6.6 Hz, 2H), 3.21 (dd, J = 12.3, 6.3 Hz, 2H), 2.03 (t, J = 6.8 Hz, 2H),1.43 (dd, J = 14.1, 7.0 Hz, 2H), 1.33- 1.09 (m, 1H), 0.80 (t, J = 7.4Hz, 3H). 79 2-{(4- ¹H NMR (400 MHz, DMSO-d₆) δ (ESI(+))fluorobenzyl)[(tetra- 9.12 (s, 1H), 8.46 (t, J = 5.7 Hz, m/e 487hydrofuran-2- 1H), 7.91 (s, 1H), 7.85 (t, J = 5.5 (M + H)⁺ylmethyl)carbamoyl]amino}- Hz, 1H), 7.81 (t, J = 1.5 Hz, 1H),N-[3-(1H-imidazol-1- 7.70 (t, J = 1.5 Hz, 1H), 7.28-yl)propyl]-1,3-thiazole-5- 7.20 (m, 2H), 7.20-7.10 (m, 2H), carboxamide5.37 (q, J = 17.1 Hz, 2H), 4.23 (t, J = 7.0 Hz, 2H), 3.87 (dd, J = 12.2,5.9 Hz, 1H), 3.28-3.17 (m, 4H), 2.08-2.00 (m, 2H), 1.82- 1.65 (m, 3H),1.42 (ddd, J = 9.1, 8.3, 6.0 Hz, 1H). 80 2-{(4-fluorobenzyl)[(1- ¹H NMR(400 MHz, DMSO-d₆) δ (ESI(+)) methoxypropan-2- 9.10 (s, 1H), 8.44 (t, J= 5.7 Hz, m/e 475 yl)carbamoyl]amino}-N-[3- 1H), 7.90 (s, 1H), 7.81 (t,J = 1.5 (M + H)⁺ (1H-imidazol-1-yl)propyl]- Hz, 1H), 7.69 (t, J = 1.4Hz, 1H), 1,3-thiazole-5-carboxamide 7.54 (d, J = 7.9 Hz, 1H), 7.31- 7.21(m, 2H), 7.21-7.09 (m, 2H), 5.36 (d, J = 2.5 Hz, 2H), 4.22 (t, J = 7.0Hz, 2H), 4.00 (dt, J = 18.2, 5.6 Hz, 1H), 3.32 (dd, J = 9.6, 6.6 Hz,2H), 3.26-3.21 (m, 5H), 2.03 (t, J = 6.8 Hz, 2H), 1.08 (d, J = 6.8 Hz,3H). 81 2-{(4- ¹H NMR (400 MHz, DMSO-d₆) δ (ESI(+))fluorobenzyl)[(tetrahydro- 9.11 (s, 1H), 8.45 (t, J = 5.7 Hz, m/e 5012H-pyran-2- 1H), 7.91 (s, 1H), 7.87-7.75 (m, (M + H)⁺ylmethyl)carbamoyl]amino}- 2H), 7.69 (t, J = 1.4 Hz, 1H), 7.24N-[3-(1H-imidazol-1- (dd, J = 8.6, 5.6 Hz, 2H), 7.20-yl)propyl]-1,3-thiazole-5- 7.09 (m, 2H), 5.36 (s, 2H), 4.22 carboxamide(dd, J = 9.0, 5.0 Hz, 2H), 3.82 (dd, J = 11.0, 2.7 Hz, 1H), 3.32- 3.24(m, 2H), 3.23-3.15 (m, 4H), 2.09-1.98 (m, 2H), 1.76-1.66 (m, 1H),1.46-1.33 (m, 4H), 1.09- 0.98 (m, 1H). 82 2-{(4-fluorobenzyl)[(2- ¹H NMR(400 MHz, DMSO-d₆) δ (ESI(+)) methoxyethyl)carbamoyl]amino}- 9.12 (s,1H), 8.46 (t, J = 5.7 Hz, m/e 461 N-[3-(1H-imidazol- 1H), 7.91 (s, 1H),7.87 (t, J = 5.1 (M + H)⁺ 1-yl)propyl]-1,3-thiazole-5- Hz, 1H), 7.82 (t,J = 1.5 Hz, 1H), carboxamide 7.70 (t, J = 1.5 Hz, 1H), 7.30- 7.20 (m,2H), 7.20-7.12 (m, 2H), 5.35 (s, 2H), 4.23 (t, J = 7.0 Hz, 2H), 3.39(dd, J = 8.4, 3.2 Hz, 2H), 3.34 (dd, J = 9.9, 4.6 Hz, 2H), 3.24-3.18 (m,5H), 2.04 (t, J = 6.8 Hz, 2H). 83 2-{[(2- ¹H NMR (400 MHz, DMSO-d₆) δ(ESI(+)) ethoxyethyl)carbamoyl](4- 9.11 (s, 1H), 8.46 (t, J = 5.6 Hz,m/e 475 fluorobenzyl)amino}-N-[3- 1H), 7.90 (s, 1H), 7.85 (t, J = 5.3(M + H)⁺ (1H-imidazol-1-yl)propyl]- Hz, 1H), 7.80 (d, J = 1.4 Hz, 1H),1,3-thiazole-5-carboxamide 7.69 (d, J = 1.4 Hz, 1H), 7.29- 7.18 (m, 2H),7.18-7.09 (m, 2H), 5.34 (s, 2H), 4.22 (t, J = 7.0 Hz, 2H), 3.41-3.38 (m,2H), 3.37 (d, J = 7.0 Hz, 2H), 3.33 (dd, J = 9.9, 4.7 Hz, 2H), 3.24-3.17(m, 2H), 2.11-1.94 (m, 2H), 1.05 (t, J = 7.0 Hz, 3H). 842-{(4-fluorobenzyl)[(1- ¹H NMR (400 MHz, DMSO-d₆) δ (ESI(+))methoxybutan-2- 9.11 (s, 1H), 8.44 (t, J = 5.8 Hz, m/e 489yl)carbamoyl]amino}-N-[3- 1H), 7.90 (s, 1H), 7.81 (d, J = 1.4 (M + H)⁺(1H-imidazol-1-yl)propyl]- Hz, 1H), 7.69 (d, J = 1.3 Hz, 1H),1,3-thiazole-5-carboxamide 7.41 (d, J = 8.2 Hz, 1H), 7.24 (dd, J = 8.6,5.6 Hz, 2H), 7.16 (t, J = 8.9 Hz, 2H), 5.39 (dd, J = 39.3, 17.0 Hz, 2H),4.22 (t, J = 7.0 Hz, 2H), 3.85-3.78 (m, 1H), 3.30 (dt, J = 9.7, 3.7 Hz,2H), 3.24-3.19 (m, 5H), 2.09-1.98 (m, 2H), 1.52 (ddd, J = 12.5, 7.2, 5.0Hz, 1H), 1.42-1.32 (m, 1H), 0.73 (t, J = 7.4 Hz, 3H). 862-{[(1,3-dioxolan-2- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+))ylmethyl)carbamoyl](4- 9.35-9.24 (m, 1H), 8.88-8.68 m/e 489fluorobenzyl)amino}-N-[3- (m, 1H), 7.94-7.85 (m, 1H), 7.39- (M + H)+(1H-imidazol-1-yl)propyl]- 7.34 (m, 1H), 7.32-7.27 (m,1,3-thiazole-5-carboxamide 3H), 7.21-7.08 (m, 1H), 7.01 (t, J = 8.6 Hz,2H), 5.21-5.09 (m, 2H), 5.06 (t, J = 3.4 Hz, 1H), 4.35- 4.25 (m, 2H),3.99-3.82 (m, 4H), 3.64 (dd, J = 5.1, 3.5 Hz, 2H), 3.44 (dt, J = 10.2,2.9 Hz, 2H), 2.24-2.19 (m, 2H). 87 2-[(4-fluorobenzyl){[2- ¹H NMR (400MHz, CDCl₃) δ (ESI(+)) (propan-2- 9.30 (ddd, J = 3.5, 2.1, 0.8 Hz, m/e489 yloxy)ethyl]carbamoyl}amino]- 1H), 8.55-8.35 (m, 1H), 7.94- (M + H)+N-[3-(1H-imidazol-1- 7.86 (m, 1H), 7.35 (s, 1H), 7.32-yl)propyl]-1,3-thiazole-5- 7.27 (m, 3H), 7.10-7.04 (m, 1H), carboxamide7.03-6.95 (m, 2H), 5.18 (s, 2H), 4.32 (dd, J = 9.5, 3.5 Hz, 2H),3.62-3.49 (m, 6H), 3.48-3.41 (m, 2H), 2.23-2.20 (m, 2H), 1.13 (t, J =4.9 Hz, 6H). 88 2-{[(1,4-dioxan-2- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+))ylmethyl)carbamoyl](4- 9.43-9.29 (m, 1H), 8.77-8.63 m/e 503fluorobenzyl)amino}-N-[3- (m, 1H), 7.98-7.88 (m, 1H), 7.35 (M + H)+(1H-imidazol-1-yl)propyl]- (s, 1H), 7.31-7.27 (m, 3H), 7.22-1,3-thiazole-5-carboxamide 7.11 (m, 1H), 7.06-6.95 (m, 2H), 5.27-5.06(m, 2H), 4.33 (ddd, J = 5.9, 4.1, 3.0 Hz, 2H), 3.82-3.73 (m, 3H),3.73-3.67 (m, 2H), 3.63-3.49 (m, 2H), 3.49- 3.39 (m, 2H), 3.39-3.25 (m,2H), 2.23-2.20 (m, 2H). 89 2-{[(1,3-dimethoxypropan- ¹H NMR (400 MHz,CDCl₃) δ (ESI(+)) 2-yl)carbamoyl](4- 9.26-9.18 (m, 1H), 8.30 (s, 1H),m/e 505 fluorobenzyl)amino}-N-[3- 7.89 (s, 1H), 7.35 (s, 1H), 7.30 (d,(M + H)+ (1H-imidazol-1-yl)propyl]- J = 1.8 Hz, 1H), 7.28 (d, J = 3.01,3-thiazole-5-carboxamide Hz, 2H), 7.13-7.04 (m, 1H), 7.02 (t, J = 8.6Hz, 2H), 5.19 (s, 2H), 4.31 (t, J = 6.4 Hz, 2H), 4.24- 4.13 (m, 1H),3.55 (dd, J = 9.5, 4.5 Hz, 2H), 3.44 (dd, J = 9.6, 5.6 Hz, 4H), 3.34 (s,6H), 2.27-2.15 (m, 2H). 90 2-{(4-fluorobenzyl)[(2- ¹H NMR (400 MHz,CDCl₃) δ (ESI(+)) methoxybutyl)carbamoyl]amino}- 9.22 (s, 1H), 8.47-8.29(m, 1H), m/e 489 N-[3-(1H-imidazol- 7.88 (s, 1H), 7.35 (s, 1H), 7.30 (s,(M + H)+ 1-yl)propyl]-1,3-thiazole-5- 1H), 7.29-7.26 (m, 2H), 7.14-carboxamide 7.05 (m, 1H), 7.02 (t, J = 8.6 Hz, 2H), 5.19 (q, J = 16.6Hz, 2H), 4.31 (t, J = 6.5 Hz, 2H), 3.68- 3.59 (m, 1H), 3.48-3.40 (m,2H), 3.32 (s, 3H), 3.30-3.23 (m, 2H), 2.27-2.15 (m, 2H), 1.66-1.53 (m,1H), 1.47 (dt, J = 13.6, 6.9 Hz, 1H), 0.93 (dd, J = 9.4, 5.6 Hz, 3H). 912-[(4- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+)) fluorobenzyl)(tetrahydrofuran-9.47-9.31 (m, 2H), 7.94-7.85 m/e 473 3-ylcarbamoyl)amino]-N- (m, 1H),7.35 (s, 1H), 7.29 (d, J = (M + H)+ [3-(1H-imidazol-1- 8.7 Hz, 3H),7.25-7.18 (m, 1H), yl)propyl]-1,3-thiazole-5- 7.08-6.95 (m, 2H), 5.12(s, 2H), carboxamide 4.59-4.50 (m, 1H), 4.33 (td, J = 5.4, 1.1 Hz, 2H),4.00-3.90 (m, 2H), 3.86 (td, J = 8.6, 5.5 Hz, 1H), 3.78 (dd, J = 9.4,2.8 Hz, 1H), 3.44 (dt, J = 8.9, 3.6 Hz, 2H), 2.35-2.28 (m, 1H), 2.26-2.20 (m, 2H), 1.96-1.87 (m, 1H). 92 2-[(4- ¹H NMR (400 MHz, CDCl₃) δ(ESI(+)) fluorobenzyl)(tetrahydro- 9.22 (s, 1H), 9.01-8.81 (m, 1H), m/e487 2H-pyran-3- 7.88 (s, 1H), 7.35 (s, 1H), 7.29 (t, (M + H)+ylcarbamoyl)amino]-N-[3- J = 6.9 Hz, 3H), 7.07 (dd, J = 8.5,(1H-imidazol-1-yl)propyl]- 3.5 Hz, 1H), 7.02 (t, J = 8.6 Hz,1,3-thiazole-5-carboxamide 2H), 5.26 (d, J = 16.7 Hz, 1H), 5.08 (d, J =16.6 Hz, 1H), 4.31 (t, J = 6.4 Hz, 2H), 3.99 (ddd, J = 8.8, 3.5, 1.6 Hz,1H), 3.83-3.78 (m, 1H), 3.64 (dddd, J = 22.5, 16.6, 7.9, 3.3 Hz, 3H),3.44 (dd, J = 11.4, 5.9 Hz, 2H), 2.29-2.14 (m, 2H), 1.91 (ddd, J = 8.1,6.4, 2.7 Hz, 1H), 1.79-1.68 (m, 1H), 1.68-1.53 (m, 2H). 1232-[(4-cyanobenzyl){[2- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+)) (propan-2-9.22-9.13 (m, 1H), 8.93-8.79 m/e 496 yloxy)ethyl]carbamoyl}amino]- (m,1H), 7.82 (s, 1H), 7.63 (d, J = (M + H)+ N-[3-(1H-imidazol-1- 8.1 Hz,2H), 7.45-7.32 (m, 3H), yl)propyl]-1,3-thiazole-5- 7.29 (s, 1H),7.07-6.96 (m, 1H), carboxamide 5.25 (s, 2H), 4.30 (t, J = 6.4 Hz, 2H),3.65-3.54 (m, 5H), 3.46- 3.40 (m, 2H), 2.23 (dd, J = 7.3, 3.9 Hz, 2H),1.15 (d, J = 6.1 Hz, 6H). 124 2-{(4-cyanobenzyl)[(2- ¹H NMR (400 MHz,CDCl₃) δ (ESI(+)) methoxypropyl)carbamoyl]amino}- 9.33-9.20 (m, 1H),8.83-8.73 m/e 482 N-[3-(1H-imidazol- (m, 1H), 7.90-7.81 (m, 1H), 7.63(M + H)+ 1-yl)propyl]-1,3-thiazole-5- (d, J = 8.2 Hz, 2H), 7.39 (dd, J =carboxamide 15.0, 7.1 Hz, 3H), 7.28 (s, 1H), 7.12-6.99 (m, 1H),5.33-5.14 (m, 2H), 4.37-4.25 (m, 2H), 4.21- 4.11 (m, 1H), 3.48-3.39 (m,4H), 3.36 (s, 3H), 2.26-2.20 (m, 2H), 1.29-1.23 (m, 3H). 1252-[(4-cyanobenzyl){[2-(2- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+))hydroxyethoxy)ethyl]carbam- 9.39-9.27 (m, 1H), 9.26-9.16 m/e 498oyl}amino]-N-[3-(1H- (m, 1H), 7.81 (s, 1H), 7.62 (d, J = (M + H)+imidazol-1-yl)propyl]-1,3- 8.2 Hz, 2H), 7.41-7.34 (m, 3H),thiazole-5-carboxamide 7.28 (s, 1H), 7.15-7.05 (m, 1H), 5.22 (s, 2H),4.55-4.5 (m, 2H), 4.36-4.29 (m, 2H), 3.85-3.75 (m, 2H), 3.67 (d, J = 4.7Hz, 3H), 3.65-3.60 (m, 2H), 3.46-3.40 (m, 2H), 2.25-2.19 (m, 2H). 1262-[(4-cyanobenzyl){[3- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+)) (propan-2-9.26-9.14 (m, 1H), 8.61 (s, 1H), m/e 510 yloxy)propyl]carbam- 7.81 (s,1H), 7.62 (d, J = 8.2 Hz, (M + H)+ oyl}amino]- 2H), 7.38 (d, J = 8.2 Hz,3H), N-[3-(1H-imidazol-1- 7.29 (s, 1H), 6.96 (s, 1H), 5.24 (s,yl)propyl]-1,3-thiazole-5- 2H), 4.35-4.30 (m, 2H), 3.53 (dt, carboxamideJ = 16.3, 5.8 Hz, 5H), 3.45-3.40 (m, 2H), 2.26-2.20 (m, 2H), 1.88- 1.82(m, 2H), 1.12 (d, J = 6.1 Hz, 6H). 127 2-{(4-cyanobenzyl)[(3- ¹H NMR(400 MHz, CDCl₃) δ (ESI(+)) hydroxy-2,2- 9.67 (s, 1H), 9.34 (s, 1H),7.87 (s, m/e 496 dimethylpropyl)carbam- 1H), 7.63 (d, J = 8.2 Hz, 2H),(M + H)+ oyl]amino}- 7.45-7.34 (m, 3H), 7.25-7.18 N-[3-(1H-imidazol- (m,1H), 5.20 (s, 2H), 4.32 (t, J = 1-yl)propyl]-1,3-thiazole-5- 6.1 Hz,2H), 4.18-4.12 (m, 2H), carboxamide 3.42 (d, J = 4.4 Hz, 2H), 3.38 (d, J= 6.1 Hz, 2H), 2.25-2.20 (m, 2H), 1.06 (s, 6H). 1282-{(4-cyanobenzyl)[(2- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+))hydroxypropyl)carbam- 9.85 (s, 1H), 9.32 (s, 1H), 7.85- m/e 468oyl]amino}- 7.74 (m, 1H), 7.63 (d, J = 8.2 Hz, (M + H)+N-[3-(1H-imidazol- 2H), 7.42-7.35 (m, 3H), 7.24 (s,1-yl)propyl]-1,3-thiazole-5- 1H), 5.39-5.29 (m, 1H), 5.28- carboxamide5.10 (m, 2H), 4.40-4.25 (m, 2H), 3.93-3.81 (m, 1H), 3.53-3.46 (m, 1H),3.46-3.36 (m, 2H), 2.27- 2.21 (m, 2H), 1.43 (d, J = 6.4 Hz, 3H). 1292-{(4-cyanobenzyl)[(1- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+))hydroxypropan-2- 9.74-9.65 (m, 1H), 9.38-9.18 m/e 468yl)carbamoyl]amino}-N-[3- (m, 1H), 7.80 (d, J = 4.4 Hz, 1H), (M + H)+(1H-imidazol-1-yl)propyl]- 7.63 (d, J = 8.3 Hz, 2H), 7.42-1,3-thiazole-5-carboxamide 7.35 (m, 3H), 7.23-7.08 (m, 1H), 5.20 (dt, J= 21.5, 9.8 Hz, 2H), 4.63-4.52 (m, 1H), 4.47-4.40 (m, 1H), 4.40-4.34 (m,1H), 4.34- 4.27 (m, 2H), 3.48-3.38 (m, 2H), 2.26-2.21 (m, 4H), 1.37 (d,J = 6.7 Hz, 3H). 130 2-{(4-cyanobenzyl)[(3- ¹H NMR (400 MHz, CDCl₃) δ(ESI(+)) hydroxypropyl)carbam- 9.58 (d, J = 4.9 Hz, 1H), 9.41 (d, J =m/e 468 oyl]amino}- 6.0 Hz, 1H), 7.90 (s, 1H), 7.63 (M + H)+N-[3-(1H-imidazol- (d, J = 8.2 Hz, 2H), 7.39 (d, J =1-yl)propyl]-1,3-thiazole-5- 8.3 Hz, 2H), 7.35 (s, 1H), 7.24 (s,carboxamide 1H), 5.19 (s, 2H), 4.47 (t, J = 6.1 Hz, 2H), 4.33 (dd, J =7.1, 5.8 Hz, 2H), 3.54 (d, J = 5.9 Hz, 2H), 3.42 (d, J = 2.0 Hz, 2H),2.27- 2.21 (m, 2H), 2.13-2.08 (m, 2H). 131 2-[(4-cyanobenzyl){[(2S)-1-¹H NMR (400 MHz, CDCl₃) δ (ESI(+)) hydroxybut-3-en-2- 10.02 (s, 1H),9.31 (s, 1H), 7.84 m/e 480 yl]carbamoyl}amino]-N-[3- (s, 1H), 7.63 (d, J= 8.2 Hz, 2H), (M + H)+ (1H-imidazol-1-yl)propyl]- 7.45-7.34 (m, 3H),7.23 (s, 1H), 1,3-thiazole-5-carboxamide 6.01-5.84 (m, 1H), 5.38 (t, J =14.8 Hz, 2H), 5.20 (dd, J = 39.0, 17.5 Hz, 2H), 4.98-4.90 (m, 1H), 4.61(dd, J = 11.2, 4.3 Hz, 1H), 4.50 (dd, J = 11.1, 5.0 Hz, 1H), 4.31 (t, J= 6.4 Hz, 2H), 3.42 (d, J = 5.8 Hz, 2H), 2.26-2.21 (m, 2H). 1322-{(4-cyanobenzyl)[(4- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+))hydroxybutyl)carbam- 9.53 (s, 1H), 9.30 (s, 1H), 7.85 (s, m/e 482oyl]amino}- 1H), 7.62 (d, J = 8.2 Hz, 2H), (M + H)+ N-[3-(1H-imidazol-1-7.39 (d, J = 8.2 Hz, 2H), 7.35 (s, yl)propyl]-1,3-thiazole-5- 1H), 5.20(s, 2H), 4.41 (t, J = 6.4 carboxamide Hz, 2H), 4.32 (t, J = 6.3 Hz, 2H),3.54-3.45 (m, 2H), 3.45-3.36 (m, 2H), 2.26-2.21 (m, 3H), 1.85 (dd, J =15.1, 6.7 Hz, 2H), 1.75 (dd, J = 14.9, 6.5 Hz, 2H). 140 2-{[(3-amino-3-¹H NMR (400 MHz, methanol-d₄) (ESI(+)) oxopropyl)carbamoyl] (4- δ 8.97(s, 1H), 7.79 (s, 1H), 7.73 m/e 481 cyanobenzyl)amino}-N-[3- (d, J = 8.2Hz, 2H), 7.69 (s, 1H), (M + H)+ (1H-imidazol-1-yl)propyl]- 7.57 (s, 1H),7.51 (d, J = 8.2 Hz, 1,3-thiazole-5-carboxamide 2H), 5.35 (s, 2H), 4.30(t, J = 6.8 Hz, 2H), 3.47 (t, J = 6.4 Hz, 2H), 3.35 (t, J = 6.4 Hz, 2H),2.41 (dd, J = 16.2, 9.2 Hz, 2H), 2.15 (p, J = 6.6 Hz, 2H). 1412-[{[3-(acetylamino)-2- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))methylpropyl]carbamoyl}(4- δ 8.96 (s, 1H), 7.76 (d, J = 9.6 Hz, m/e 523cyanobenzyl)amino]-N-[3- 2H), 7.73 (s, 1H), 7.69 (s, 1H), (M + H)+(1H-imidazol-1-yl)propyl]- 7.57 (s, 1H), 7.52 (d, J = 8.1 Hz,1,3-thiazole-5-carboxamide 2H), 5.36 (s, 2H), 4.30 (t, J = 6.8 Hz, 2H),3.35 (t, J = 6.4 Hz, 2H), 3.10 (d, J = 6.4 Hz, 4H), 2.14 (p, J = 6.5 Hz,2H), 1.95 (s, 3H), 1.85 (dd, J = 12.9, 6.4 Hz, 1H), 0.92 (d, J = 6.8 Hz,3H). 142 2-[(4-cyanobenzyl){[3- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))(dimethylamino)-3- δ 8.97 (s, 1H), 7.78 (s, 1H), 7.73 m/e 509oxopropyl]carbamoyl}amino]- (d, J = 8.3 Hz, 2H), 7.70 (s, 1H), (M + H)+N-[3-(1H-imidazol-1- 7.57 (s, 1H), 7.49 (d, J = 8.0 Hz,yl)propyl]-1,3-thiazole-5- 2H), 5.34 (s, 2H), 4.30 (t, J = 6.8carboxamide Hz, 2H), 3.47 (t, J = 6.8 Hz, 2H), 3.35 (t, J = 6.4 Hz, 2H),3.03 (s, 3H), 2.92 (s, 3H), 2.64 (d, J = 14.3 Hz, 2H), 2.22-2.07 (m, 2H)143 2-{(4-cyanobenzyl)[(3- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))ethoxy-2- δ 8.96 (s, 1H), 7.78 (s, 1H), 7.73 m/e 512hydroxypropyl)carbam- (t, J = 7.2 Hz, 2H), 7.69 (s, 1H), (M + H)+oyl]amino}- 7.57 (s, 1H), 7.51 (d, J = 8.1 Hz, N-[3-(1H-imidazol- 2H),5.36 (s, 2H), 4.30 (t, J = 6.8 1-yl)propyl]-1,3-thiazole-5- Hz, 2H),3.82 (t, J = 4.8 Hz, 1H), carboxamide 3.52 (q, J = 7.1 Hz, 2H), 3.48-3.38 (m, 2H), 3.35 (d, J = 6.6 Hz, 2H), 3.22 (dd, J = 13.7, 7.0 Hz, 2H),2.15 (t, J = 6.6 Hz, 2H), 1.18 (t, J = 7.1 Hz, 3H). 1442-[(4-cyanobenzyl){[3- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))(diethylamino)propyl]carbam- δ 8.97 (s, 1H), 7.85 (s, 1H), 7.73 m/e 523oyl}amino]-N-[3-(1H- (d, J = 8.2 Hz, 2H), 7.70 (s, 1H), (M + H)+imidazol-1-yl)propyl]-1,3- 7.57 (s, 1H), 7.50 (d, J = 8.2 Hz,thiazole-5-carboxamide 2H), 5.36 (s, 2H), 4.31 (t, J = 6.9 Hz, 2H), 3.35(dd, J = 11.6, 5.0 Hz, 4H), 3.23 (q, J = 7.3 Hz, 4H), 3.18-3.11 (m, 2H),2.15 (p, J = 6.8 Hz, 2H), 2.03-1.85 (m, 2H), 1.31 (t, J = 7.3 Hz, 6H).145 2-[{[2- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))(acetylamino)ethyl]carbam- δ 8.97 (s, 1H), 7.79 (s, 1H), 7.74 m/e 495oyl}(4-cyanobenzyl)amino]- (d, J = 8.2 Hz, 2H), 7.69 (s, 1H), (M + H)+N-[3-(1H-imidazol-1- 7.57 (s, 1H), 7.51 (d, J = 8.1 Hz,yl)propyl]-1,3-thiazole-5- 2H), 5.35 (s, 2H), 4.30 (t, J = 6.8carboxamide Hz, 2H), 3.35 (t, J = 6.5 Hz, 2H), 2.22-2.07 (m, 2H), 1.93(s, 3H). 146 2-[(4-cyanobenzyl){[2- ¹H NMR (400 MHz, methanol-d₄)(ESI(+)) (diethylamino)ethyl]carbam- δ 8.97 (s, 1H), 7.87 (s, 1H), 7.74m/e 509 oyl}amino]-N-[3-(1H- (d, J = 8.2 Hz, 2H), 7.70 (s, 1H), (M + H)+imidazol-1-yl)propyl]-1,3- 7.58 (s, 1H), 7.49 (d, J = 8.2 Hz,thiazole-5-carboxamide 2H), 5.37 (s, 2H), 4.31 (t, J = 6.9 Hz, 2H), 3.56(t, J = 5.9 Hz, 2H), 3.35 (t, J = 6.5 Hz, 2H), 3.27 (dd, J = 7.3, 2.8Hz, 4H), 2.15 (t, J = 6.7 Hz, 2H), 1.33 (t, J = 7.3 Hz, 6H). 1472-[(4-cyanobenzyl)({2-[(2- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))methylpropanoyl)amino]eth- δ 8.96 (s, 1H), 7.78 (s, 1H), 7.73 m/e 523yl}carbamoyl)amino]-N-[3- (d, J = 8.2 Hz, 2H), 7.69 (s, 1H), (M + H)+(1H-imidazol-1-yl)propyl]- 7.57 (s, 1H), 7.50 (d, J = 8.2 Hz,1,3-thiazole-5-carboxamide 2H), 5.34 (s, 2H), 4.29 (t, J = 6.8 Hz, 2H),3.34 (t, J = 6.5 Hz, 2H), 2.39 (dt, J = 13.9, 7.0 Hz, 1H), 2.14 (p, J =6.6 Hz, 2H), 1.07 (d, J = 6.9 Hz, 6H). 148 2-[(4-cyanobenzyl){[(2R)-1-¹H NMR (400 MHz, methanol-d₄) (ESI(+)) hydroxybut-3-en-2- δ 8.96 (s,1H), 7.78 (s, 1H), 7.74 m/e 480 yl]carbamoyl}amino]-N-[3- (d, J = 8.2Hz, 2H), 7.69 (s, 1H), (M + H)+ (1H-imidazol-1-yl)propyl]- 7.57 (s, 1H),7.52 (d, J = 8.1 Hz, 1,3-thiazole-5-carboxamide 2H), 5.97-5.81 (m, 1H),5.47- 5.31 (m, 2H), 5.24 (d, J = 17.0 Hz, 1H), 5.16 (d, J = 10.6 Hz,1H), 4.39-4.33 (m, 1H), 4.30 (t, J = 6.8 Hz, 2H), 3.64-3.50 (m, 2H),3.35 (t, J = 6.4 Hz, 2H), 2.14 (p, J = 6.8 Hz, 2H). 1492-[(4-cyanobenzyl){[3-(3- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))hydroxyazetidin-1- δ 8.97 (s, 1H), 7.84 (s, 1H), 7.74 m/e 523yl)propyl]carbamoyl}amino]- (d, J = 8.2 Hz, 2H), 7.69 (d, J = (M + H)+N-[3-(1H-imidazol-1- 1.5 Hz, 1H), 7.58 (t, J = 1.6 Hz,yl)propyl]-1,3-thiazole-5- 1H), 7.50 (d, J = 8.0 Hz, 2H), carboxamide5.36 (s, 2H), 4.68-4.58 (m, 1H), 4.47 (dd, J = 10.2, 8.2 Hz, 1H), 4.30(t, J = 6.9 Hz, 2H), 4.26- 4.14 (m, 1H), 4.06 (d, J = 8.9 Hz, 1H),3.87-3.79 (m, 1H), 3.35 (t, J = 6.5 Hz, 2H), 3.27 (t, J = 6.7 Hz, 3H),3.23-3.16 (m, 1H), 2.15 (p, J = 6.7 Hz, 2H), 1.80 (dt, J = 13.9, 7.1 Hz,2H). 159 ethyl N-[(4-cyanobenzyl)(5- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+)){[3-(1H-imidazol-1- 9.15 (s, 1H), 8.04-7.96 (m, 1H), m/e 510yl)propyl]carbamoyl}-1,3- 7.96-7.84 (m, 1H), 7.64 (d, J = (M + H)+thiazol-2-yl)carbamoyl]- 8.2 Hz, 2H), 7.37 (d, J = 8.1 Hz,beta-alaninate 2H), 7.31 (s, 1H), 5.50-5.36 (m, 2H), 4.33 (t, J = 6.2Hz, 2H), 4.14 (q, J = 7.2 Hz, 2H), 3.57 (t, J = 6.2 Hz, 2H), 3.41 (td, J= 5.6, 1.0 Hz, 2H), 2.61-2.51 (m, 2H), 2.21 (qd, J = 6.8, 3.4 Hz, 2H),1.25 (t, J = 7.2 Hz, 3H). 160 ethyl 4-{[(4- ¹H NMR (400 MHz, CDCl₃) δ(ESI(+)) cyanobenzyl)(5-{[3-(1H- 9.39 (s, 1H), 8.00 (d, J = 46.6 Hz, m/e524 imidazol-1- 1H), 7.71-7.60 (m, 2H), 7.44- (M + H)+yl)propyl]carbamoyl}-1,3- 7.34 (m, 3H), 7.28 (d, J = 1.5 Hz,thiazol-2-yl)carbam- 1H), 5.50-5.42 (m, 1H), 4.41- oyl]amino}butanoate4.31 (m, 2H), 4.18-4.05 (m, 2H), 3.46-3.37 (m, 2H), 3.38-3.26 (m, 2H),2.39-2.34 (m, 3H), 2.24- 2.20 (m, 3H), 1.96-1.82 (m, 2H), 1.33-1.18 (m,3H). 161 ethyl 3-{[(4- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+))cyanobenzyl)(5-{[3-(1H- 9.15 (s, 1H), 8.09-8.00 (m, 1H), m/e 524imidazol-1- 7.65 (d, J = 8.2 Hz, 2H), 7.39 (dd, (M + H)+yl)propyl]carbamoyl}-1,3- J = 11.3, 4.8 Hz, 3H), 7.33 (s,thiazol-2-yl)carbam- 1H), 5.54-5.47 (m, 2H), 4.40- oyl]amino}butanoate4.23 (m, 3H), 4.12 (q, J = 7.1 Hz, 2H), 3.42 (dd, J = 10.1, 5.1 Hz, 2H),2.65-2.43 (m, 2H), 2.28- 2.18 (m, 2H), 1.29-1.18 (m, 6H). 162 ethyl3-{[(4- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+)) cyanobenzyl)(5-{[3-(1H- 9.13(s, 1H), 8.10 (dd, J = 6.0, 1.4 m/e 552 imidazol-1- Hz, 1H), 8.05 (s,1H), 7.65 (d, J = (M + H)+ yl)propyl]carbamoyl}-1,3- 8.2 Hz, 2H), 7.39(d, J = 8.6 Hz, thiazol-2- 3H), 7.33 (d, J = 7.9 Hz, 1H),yl)carbamoyl]amino}-4- 7.04-6.94 (m, 1H), 5.48 (d, J = methylpentanoate24.0 Hz, 2H), 5.35-5.26 (m, 1H), 4.33 (t, J = 6.3 Hz, 2H), 4.16- 3.94(m, 3H), 3.46-3.34 (m, 2H), 2.64-2.41 (m, 2H), 2.26-2.15 (m, 2H), 1.20(t, J = 7.1 Hz, 3H), 0.93 (d, J = 6.5 Hz, 6H). 163 ethyl 3-{[(4- ¹H NMR(400 MHz, CDCl₃) δ (ESI(+)) cyanobenzyl)(5-{[3-(1H- 9.21-9.08 (m, 1H),8.06-7.96 m/e 538 imidazol-1- (m, 1H), 7.91 (dd, J = 5.9, 1.8 Hz, (M +H)+ yl)propyl]carbamoyl}-1,3- 1H), 7.65 (d, J = 8.1 Hz, 2H), thiazol-2-7.38 (d, J = 8.2 Hz, 3H), 7.31 (s, yl)carbamoyl]amino}-2,2- 1H),6.90-6.64 (m, 1H), 5.44 (d, dimethylpropanoate J = 20.7 Hz, 2H), 4.33(t, J = 6.1 Hz, 2H), 4.18-4.08 (m, 2H), 3.49- 3.37 (m, 4H), 2.24-2.13(m, 2H), 1.31-1.17 (m, 9H). 164 3-{[(4-cyanobenzyl)(5-{[3- ¹H NMR (400MHz, methanol-d₄) (ESI(+)) (1H-imidazol-1- δ 8.97 (s, 1H), 7.80 (s, 1H),7.74 m/e 508 yl)propyl]carbamoyl}-1,3- (d, J = 8.0 Hz, 2H), 7.69 (s,1H), (M + H)+ thiazol-2- 7.57 (s, 1H), 7.52 (d, J = 7.9 Hz,yl)carbamoyl]amino}cyclo- 2H), 5.37 (d, J = 9.8 Hz, 2H),butanecarboxylic acid 4.30 (t, J = 6.8 Hz, 2H), 4.26- 4.11 (m, 1H), 3.34(d, J = 3.4 Hz, 2H), 2.80 (d, J = 8.4 Hz, 1H), 2.55 (d, J = 8.1 Hz, 2H),2.25- 2.04 (m, 4H). 165 ethyl 3-{[(4- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+))cyanobenzyl)(5-{[3-(1H- 9.26 (s, 1H), 7.94 (s, 1H), 7.78 m/e 524imidazol-1- (ddd, J = 3.7, 2.7, 2.0 Hz, 1H), (M + H)+yl)propyl]carbamoyl}-1,3- 7.64 (d, J = 8.1 Hz, 2H), 7.38 (d, J =thiazol-2- 7.2 Hz, 3H), 7.29 (s, 1H), 6.52 yl)carbamoyl]amino}-2- (d, J= 1.6 Hz, 1H), 5.37 (s, 2H), methylpropanoate 4.34 (t, J = 6.2 Hz, 2H),4.21- 4.07 (m, 2H), 3.46-3.33 (m, 4H), 2.75-2.68 (m, 1H), 2.24-2.15 (m,2H), 1.33-1.12 (m, 6H). 166 2-{(4-cyanobenzyl)[(3- ¹H NMR (400 MHz,CDCl₃) δ (ESI(+)) methoxypropyl)carbam- 8.96 (s, 1H), 7.75 (d, J = 5.6Hz, m/e 482 oyl]amino}- 2H), 7.73 (s, 1H), 7.69 (s, 1H), (M + H)+N-[3-(1H-imidazol- 7.57 (s, 1H), 7.51 (d, J = 8.2 Hz,1-yl)propyl]-1,3-thiazole-5- 2H), 5.35 (s, 2H), 4.33-4.24 (m,carboxamide 2H), 3.44 (t, J = 6.3 Hz, 2H), 3.39- 3.34 (m, 3H), 3.28-3.23(m, 2H), 2.20-2.08 (m, 2H), 1.84- 1.72 (m, 2H). 1673-{[(4-cyanobenzyl)(5-{[3- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))(1H-imidazol-1- δ 8.97 (s, 1H), 7.75 (d, J = 6.1 Hz, m/e 496yl)propyl]carbamoyl}-1,3- 2H), 7.72 (s, 1H), 7.69 (s, 1H), (M + H)+thiazol-2-yl)carbam- 7.57 (s, 1H), 7.51 (d, J = 8.2 Hz,oyl]amino}butanoic 2H), 5.35 (s, 2H), 4.30 (t, J = 6.8 acid Hz, 3H),4.25-4.12 (m, 1H), 3.39- 3.33 (m, 2H), 2.59 (dd, J = 15.3, 6.2 Hz, 1H),2.42 (dd, J = 15.3, 7.0 Hz, 1H), 2.20-2.09 (m, 2H), 1.23 (d, J = 6.7 Hz,3H). 168 3-{[(4-cyanobenzyl)(5-{[3- ¹H NMR (400 MHz, methanol-d₄)(ESI(+)) (1H-imidazol-1- δ 8.96 (s, 1H), 7.73 (d, J = 8.3 Hz, m/e 524yl)propyl]carbamoyl}-1,3- 3H), 7.69 (s, 1H), 7.57 (s, 1H), (M + H)+thiazol-2- 7.52 (d, J = 8.2 Hz, 2H), 5.37 (dt, yl)carbamoyl]amino}-4- J= 26.9, 11.8 Hz, 2H), 4.36- methylpentanoic acid 4.24 (m, 2H), 4.08-3.93(m, 1H), 3.35 (d, J = 6.6 Hz, 2H), 2.54 (dd, J = 15.4, 5.1 Hz, 1H),2.49-2.38 (m, 1H), 2.22-2.07 (m, 2H), 1.91- 1.79 (m, 1H), 0.94 (dd, J =6.7, 2.6 Hz, 6H). 169 3-{[(4-cyanobenzyl)(5-{[3- ¹H NMR (400 MHz,methanol-d₄) (ESI(+)) (1H-imidazol-1- δ 8.96 (s, 1H), 7.80-7.71 (m, m/e510 yl)propyl]carbamoyl}-1,3- 3H), 7.69 (s, 1H), 7.57 (s, 1H), (M + H)+thiazol-2- 7.51 (d, J = 8.2 Hz, 2H), 5.37 (s, yl)carbamoyl]amino}-2,2-2H), 4.29 (t, J = 6.8 Hz, 2H), 3.43- dimethylpropanoic acid 3.32 (m,4H), 2.22-2.07 (m, 2H), 1.18 (s, 6H). 170 3-{[(4-cyanobenzyl)(5-{[3- ¹HNMR (400 MHz, methanol-d₄) (ESI(+)) (1H-imidazol-1- δ 8.96 (s, 1H),7.81-7.71 (m, m/e 496 yl)propyl]carbamoyl}-1,3- 3H), 7.69 (s, 1H), 7.57(s, 1H), (M + H)+ thiazol-2- 7.51 (d, J = 8.1 Hz, 2H), 5.35 (s,yl)carbamoyl]amino}-2- 2H), 4.30 (t, J = 6.8 Hz, 2H), 3.50-methylpropanoic acid 3.33 (m, 4H), 2.75-2.61 (m, 1H), 2.15 (dd, J =12.9, 6.4 Hz, 2H), 1.17 (d, J = 7.2 Hz, 3H) 171N-[(4-cyanobenzyl)(5-{[3- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))(1H-imidazol-1- δ 8.97 (s, 1H), 7.77 (s, 1H), 7.73 m/e 482yl)propyl]carbamoyl}-1,3- (d, J = 8.2 Hz, 2H), 7.70 (s, 1H), (M + H)+thiazol-2-yl)carbamoyl]- 7.57 (s, 1H), 7.51 (d, J = 8.2 Hz, beta-alanine2H), 5.35 (s, 2H), 4.30 (t, J = 6.8 Hz, 2H), 3.46 (t, J = 6.8 Hz, 2H),3.39-3.33 (m, 2H), 2.54 (t, J = 6.8 Hz, 2H), 2.22-2.08 (m, 2H). 1724-{[(4-cyanobenzyl)(5-{[3- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))(1H-imidazol-1- δ 8.97 (s, 1H), 7.77 (s, 1H), 7.74 m/e 496yl)propyl]carbamoyl}-1,3- (d, J = 8.2 Hz, 2H), 7.70 (s, 1H), (M + H)+thiazol-2-yl)carbam- 7.57 (s, 1H), 7.52 (d, J = 8.1 Hz,oyl]amino}butanoic 2H), 5.35 (s, 2H), 4.30 (t, J = 6.8 acid Hz, 2H),3.39-3.33 (m, 2H), 3.24 (t, J = 6.9 Hz, 2H), 2.34 (t, J = 7.5 Hz, 2H),2.14 (dd, J = 8.4, 4.9 Hz, 2H), 1.81 (dd, J = 8.4, 5.9 Hz, 2H).

Example 92-{(4-fluorobenzyl)[2-(pyrrolidin-1-yl)ethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide

Example 6B (0.018 g, 0.05 mmol) was dissolved in acetonitrile (0.5 ml),and treated with potassium carbonate (0.021 g, 0.15 mmol) and1-(2-chloroethyl)pyrrolidine (0.017 g, 0.1 mmol). The reaction mixturewas heated via microwave at 180° C. for 30 minutes, concentrated invacuo, and submitted to reverse-phase HPLC (as described in Example 6C)to provide the title compound. ¹H NMR (400 MHz, CDCl₃) δ 10.78 (s, 1H),9.07 (s, 1H), 7.94 (s, 1H), 7.33 (dd, J=8.7, 5.1 Hz, 3H), 7.11 (s, 1H),7.04 (t, J=8.6 Hz, 2H), 4.48-4.38 (m, 4H), 4.30 (t, J=5.8 Hz, 2H), 3.41(dd, J=11.1, 5.5 Hz, 2H), 2.88 (d, J=5.4 Hz, 2H), 2.65-2.55 (m, 4H),2.20-2.19 (m, 3H), 1.78 (t, J=3.2 Hz, 5H); MS (ESI(+)) m/e 456.6 (M+H)+.

The following examples were prepared as described in Example 6B followedby Example 9, substituting the appropriate amine in Example 6B and theappropriate alkyl halide in Example 9. Title compounds were purified byeither flash chromatography (silica gel column eluting with a gradientof 0-10% methanol in dichloromethane) or reverse-phase HPLC (as inExample 6C). Accordingly, some examples were isolated as trifluoroaceticacid salts.

EX NAME ¹H NMR DATA MS DATA 7 2-{(4-fluorobenzyl)[3- ¹H NMR (400 MHz,CDCl₃) δ (ESI(+)) (morpholin-4- 10.52 (s, 1H), 8.75 (d, J = 5.5 Hz, m/e487 yl)propyl]amino}-N-[3-(1H- 1H), 7.85 (s, 1H), 7.33 (dd, J = (M + H)⁺imidazol-1-yl)propyl]-1,3- 8.5, 5.3 Hz, 2H), 7.20 (s, 1H),thiazole-5-carboxamide 7.10 (s, 1H), 7.04 (t, J = 8.6 Hz, 2H), 4.47-4.37(m, 4H), 4.25 (t, J = 7.0 Hz, 2H), 3.74-3.66 (m, 5H), 3.42 (dd, J =11.2, 5.6 Hz, 2H), 2.44-2.36 (m, 4H), 2.34 (t, J = 6.6 Hz, 2H), 2.22(dd, J = 11.3, 5.7 Hz, 2H), 2.02-1.91 (m, 2H). 8 2-{(4-fluorobenzyl)[3-¹H NMR (400 MHz, CDCl₃) δ (ESI(+)) (piperidin-1- 10.69 (s, 1H), 8.90 (s,1H), 7.90 m/e 485 yl)propyl]amino}-N-[3-(1H- (s, 1H), 7.33 (dd, J = 8.5,5.3 Hz, (M + H)⁺ imidazol-1-yl)propyl]-1,3- 2H), 7.21 (s, 1H), 7.15 (s,1H), thiazole-5-carboxamide 7.04 (t, J = 8.6 Hz, 2H), 4.42 (d, J = 10.4Hz, 4H), 4.26 (t, J = 7.0 Hz, 2H), 3.42 (dd, J = 11.1, 5.6 Hz, 2H), 2.44(d, J = 27.4 Hz, 4H), 2.26-2.18 (m, 2H), 2.02- 1.93 (m, 4H), 1.64-1.61(m, 4H), 1.46-1.5 (m, 2H). 10 2-[(4-fluorobenzyl){2-[4- ¹H NMR (400 MHz,CDCl₃) δ (ESI(+)) (propan-2-yl)piperazin-1- 7.56 (s, 1H), 7.48 (s, 1H),7.32 m/e 514 yl]ethyl}amino]-N-[3-(1H- (dd, J = 8.5, 5.5 Hz, 2H), 7.07(s, (M + H)+ imidazol-1-yl)propyl]-1,3- 1H), 7.01 (t, J = 8.7 Hz, 2H),6.97 thiazole-5-carboxamide (s, 1H), 4.24 (s, 2H), 4.04 (t, J = 6.9 Hz,2H), 3.93 (t, J = 6.1 Hz, 2H), 3.39 (d, J = 6.3 Hz, 2H), 2.85-2.78 (m,2H), 2.75-2.65 (m, 5H), 2.10-2.05 (m, 4H), 1.11 (d, J = 6.4 Hz, 6H). 142-{[(5-chloro-1,3- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+))benzodioxol-4-yl)methyl](4- 11.17 (s, 1H), 9.15 (t, J = 5.6 Hz, m/e 529fluorobenzyl)amino}-N-[3- 1H), 7.99 (s, 1H), 7.38-7.29 (m, (M + H)+(1H-imidazol-1-yl)propyl]- 2H), 7.14 (s, 1H), 7.09 (dt, J =1,3-thiazole-5-carboxamide 11.7, 1.7 Hz, 2H), 7.06-6.98 (m, 2H), 6.86(s, 1H), 6.02 (s, 2H), 5.38 (s, 2H), 4.45 (s, 2H), 4.43- 4.38 (m, 2H),3.41 (dd, J = 11.0, 5.6 Hz, 2H), 2.28-2.14 (m, 2H), 2.06 (s, 6H). 152-[(4-chlorobenzyl)(4- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+))fluorobenzyl)amino]-N-[3- 11.45 (s, 1H), 9.23 (dd, J = 7.2, m/e 484(1H-imidazol-1-yl)propyl]- 3.6 Hz, 1H), 8.02 (s, 1H), 7.43- (M + H)+1,3-thiazole-5-carboxamide 7.36 (m, 2H), 7.36-7.31 (m, 2H), 7.29 (t, J =5.4 Hz, 2H), 7.13 (t, J = 1.7 Hz, 1H), 7.09-6.95 (m, 2H), 6.89 (t, J =1.7 Hz, 1H), 5.34 (s, 2H), 4.45 (s, 2H), 4.45-4.37 (m, 2H), 3.48-3.35(m, 2H), 2.29- 2.17 (m, 2H). 16 2-[(2-chlorobenzyl)(4- ¹H NMR (400 MHz,CDCl₃) δ (ESI(+)) fluorobenzyl)amino]-N-[3- 11.25 (s, 1H), 9.21-9.12 (m,1H), m/e 484 (1H-imidazol-1-yl)propyl]- 8.03 (s, 1H), 7.62 (dd, J = 6.8,2.4 (M + H)+ 1,3-thiazole-5-carboxamide Hz, 1H), 7.46-7.41 (m, 1H),7.40- 7.30 (m, 4H), 7.10 (dt, J = 12.9, 1.6 Hz, 2H), 7.06-6.98 (m, 2H),5.50 (s, 2H), 4.45 (s, 2H), 4.42 (d, J = 6.1 Hz, 2H), 3.41 (dd, J =11.1, 5.6 Hz, 2H), 2.22 (ddd, J = 7.4, 5.9, 2.1 Hz, 2H). 172-[(2,5-dichlorobenzyl)(4- ¹H NMR (400 MHz, DMSO-d₆) δ (ESI(+))fluorobenzyl)amino]-N-[3- 9.23 (s, 1H), 8.61 (t, J = 6.0 Hz, m/e 519(1H-imidazol-1-yl)propyl]- 1H), 8.25 (t, J = 5.8 Hz, 1H), 7.81 (M + H)+1,3-thiazole-5-carboxamide (t, J = 1.7 Hz, 1H), 7.75 (t, J = 1.7 Hz,1H), 7.63 (s, 1H), 7.59-7.55 (m, 2H), 7.53 (dd, J = 8.6, 2.4 Hz, 1H),7.34 (dd, J = 8.6, 5.6 Hz, 2H), 7.15 (dd, J = 12.3, 5.5 Hz, 2H), 5.47(s, 2H), 4.41 (d, J = 5.1 Hz, 2H), 4.18 (t, J = 7.0 Hz, 2H), 3.15 (s,2H), 1.98 (t, J = 6.8 Hz, 2H). 23 2-[(4-fluorobenzyl)(4- ¹H NMR (400MHz, DMSO-d₆) δ (ESI(+)) methylbenzyl)amino]-N-[3- 9.10 (d, J = 1.2 Hz,1H), 8.28 (t, J = m/e 464 (1H-imidazol-1-yl)propyl]- 5.7 Hz, 1H), 7.79(dd, J = 5.8, (M + H)+ 1,3-thiazole-5-carboxamide 4.1 Hz, 2H), 7.68 (t,J = 1.6 Hz, 1H), 7.38-7.27 (m, 2H), 7.21- 7.11 (m, 6H), 4.72 (s, 2H),4.68 (s, 2H), 4.20 (d, J = 7.0 Hz, 2H), 3.18 (q, J = 6.6 Hz, 3H), 2.01(p, J = 6.8 Hz, 2H). 47 2-[(4-fluorobenzyl)(3- ¹H NMR (400 MHz, DMSO-d₆)δ (ESI(+)) methylbutyl)amino]-N-[3- 9.11 (s, 1H), 8.27 (t, J = 5.7 Hz,m/e 430 (1H-imidazol-1-yl)propyl]- 1H), 7.81 (d, J = 1.4 Hz, 1H), (M +H)+ 1,3-thiazole-5-carboxamide 7.75 (s, 1H), 7.69 (t, J = 1.5 Hz, 1H),7.33 (dd, J = 8.6, 5.6 Hz, 2H), 7.23-7.08 (m, 2H), 4.69 (s, 2H), 4.22(t, J = 7.0 Hz, 2H), 3.46- 3.42 (m, 2H), 3.19 (dd, J = 11.6, 5.5 Hz,2H), 2.02 (p, J = 6.8 Hz, 2H), 1.54 (dt, J = 12.9, 6.5 Hz, 1H), 1.46(dd, J = 15.0, 7.1 Hz, 2H), 0.88 (d, J = 6.4 Hz, 6H). 552-[(2-fluorobenzyl)(3- ¹H NMR (400 MHz, DMSO- (ESI(+))methylbutyl)amino]-N-[3- d6/D₂O) δ 9.22 (s, 1H), 7.78 (t, J = m/e 430(1H-imidazol-1-yl)propyl]- 1.7 Hz, 1H), 7.73 (t, J = 1.7 Hz, (M + H)+1,3-thiazole-5-carboxamide 1H), 7.67 (s, 1H), 7.53-7.46 (m, 2H),7.33-7.26 (m, 2H), 5.48 (s, 2H), 4.21 (t, J = 7.0 Hz, 2H), 3.31- 3.22(m, 2H), 3.20 (t, J = 6.6 Hz, 2H), 2.10-1.95 (m, 2H), 1.63 (dt, J =13.3, 6.7 Hz, 1H), 1.45 (dd, J = 14.4, 7.0 Hz, 2H), 0.89 (d, J = 6.6 Hz,6H). 56 2-[(3-fluorobenzyl)(3- ¹H NMR (400 MHz, DMSO- (ESI(+))methylbutyl)amino]-N-[3- d6/D₂O) δ 9.03 (s, 1H), 7.74 (d, J = m/e 430(1H-imidazol-1-yl)propyl]- 2.1 Hz, 2H), 7.64 (s, 1H), 7.41 (M + H)+1,3-thiazole-5-carboxamide (dd, J = 14.1, 7.9 Hz, 1H), 7.10 (dd, J =17.6, 9.2 Hz, 3H), 4.73 (s, 2H), 4.22 (t, J = 7.0 Hz, 2H), 3.54- 3.42(m, 2H), 3.20 (t, J = 6.5 Hz, 2H), 2.03 (t, J = 6.8 Hz, 2H), 1.59-1.51(m, 1H), 1.50-1.43 (m, 2H), 0.88 (d, J = 6.4 Hz, 6H). 572-[(2-chlorobenzyl)(3- ¹H NMR (400 MHz, DMSO- (ESI(+))methylbutyl)amino]-N-[3- d6/D₂O) δ 9.22 (s, 1H), 7.80 (t, J = m/e 447(1H-imidazol-1-yl)propyl]- 1.7 Hz, 1H), 7.71 (t, J = 1.7 Hz, (M + H)+1,3-thiazole-5-carboxamide 1H), 7.67 (s, 1H), 7.57 (d, J = 7.5 Hz, 1H),7.51-7.42 (m, 3H), 5.51 (s, 2H), 4.22 (t, J = 7.0 Hz, 2H), 3.28-3.23 (m,2H), 3.20 (t, J = 6.7 Hz, 2H), 2.03 (p, J = 6.7 Hz, 2H), 1.63 (dt, J =13.3, 6.7 Hz, 1H), 1.45 (dd, J = 14.4, 7.0 Hz, 2H), 0.89 (d, J = 6.6 Hz,6H). 58 2-[(3-chlorobenzyl)(3- ¹H NMR (400 MHz, DMSO- (ESI(+))methylbutyl)amino]-N-[3- d6/D₂O) δ 9.02 (s, 1H), 7.74 (s, m/e 447(1H-imidazol-1-yl)propyl]- 2H), 7.63 (s, 1H), 7.39 (dd, J = (M + H)+1,3-thiazole-5-carboxamide 13.9, 6.6 Hz, 3H), 7.32 (s, 1H), 7.25 (d, J =7.4 Hz, 1H), 4.72 (s, 2H), 4.22 (t, J = 7.0 Hz, 2H), 3.47 (d, J = 7.1Hz, 2H), 3.20 (t, J = 6.5 Hz, 2H), 2.09-1.97 (m, 2H), 1.54 (d, J = 6.2Hz, 1H), 1.50- 1.44 (m, 2H), 0.88 (d, J = 6.4 Hz, 6H). 592-[(4-chlorobenzyl)(3- ¹H NMR (400 MHz, DMSO- (ESI(+))methylbutyl)amino]-N-[3- d6/D₂O) δ 7.73 (s, 2H), 7.62 (s, m/e 447(1H-imidazol-1-yl)propyl]- 1H), 7.41 (d, J = 8.5 Hz, 3H), (M + H)+1,3-thiazole-5-carboxamide 7.38 (s, 1H), 7.30 (d, J = 8.5 Hz, 2H), 4.69(s, 2H), 4.21 (t, J = 7.1 Hz, 2H), 3.47 (dd, J = 11.5, 4.4 Hz, 2H), 3.19(t, J = 6.6 Hz, 2H), 2.03 (t, J = 6.8 Hz, 2H), 1.53 (d, J = 6.7 Hz, 1H),1.5 1-1.44 (m, 2H), 0.88 (d, J = 6.4 Hz, 6H). 60 2-[(4-cyanobenzyl)(3-¹H NMR (400 MHz, DMSO- (ESI(+)) methylbutyl)amino]-N-[3- d6/D₂O) δ7.85-7.78 (m, 3H), m/e 437 (1H-imidazol-1-yl)propyl]- 7.74 (s, 1H), 7.72(s, 1H), 7.64 (s, (M + H)+ 1,3-thiazole-5-carboxamide 1H), 7.46 (d, J =8.2 Hz, 2H), 4.80 (s, 2H), 4.22 (t, J = 6.9 Hz, 2H), 3.49 (m, 2H), 3.19(t, J = 6.7 Hz, 2H), 2.09-1.97 (m, 2H), 1.55 (s, 1H), 1.48 (d, J = 8.4Hz, 2H), 0.89 (d, J = 6.4 Hz, 6H).

Example 182-{(4-fluorobenzyl)[2-(methylamino)-2-oxoethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide

Example 6B (0.018 g, 0.05 mmol) was dissolved in DMSO:CH₃OH 1:1 (0.5ml), Hunig's base (0.02 mL, 0.15 mmol) and 2-chloro-N-methylacetamide(0.006 g, 0.6 mmol). The reaction mixture was heated at 80° C. overnightand submitted to reverse-phase HPLC (as described in Example 6C) toafford the title compound. ¹H NMR (400 MHz, methanol-d₄) δ 7.70 (d,J=1.9 Hz, 1H), 7.64 (s, 1H), 7.59 (d, J=1.9 Hz, 1H), 7.36 (dd, J=8.4,5.5 Hz, 2H), 7.06 (t, J=8.7 Hz, 2H), 4.97 (s, 2H), 4.48 (s, 2H), 4.29(t, J=6.9 Hz, 2H), 3.35 (t, J=6.4 Hz, 2H), 2.79 (s, 3H), 2.14 (p, J=6.7Hz, 2H); MS (ESI(+)) m/e 431 (M+H)+.

The following examples were prepared as described in Example 18,substituting the appropriate chloro-acetamide. Title compounds werepurified by either flash chromatography (silica gel column eluting witha gradient of 0-10% methanol in dichloromethane) or reverse-phase HPLC(as described in Example 6C). Accordingly, some examples were isolatedas trifluoroacetic acid salts.

EX NAME ¹H NMR DATA MS DATA 19 2-{(4-fluorobenzyl)[2-oxo- ¹H NMR (400MHz, CDCl₃) δ (ESI(+)) 2-(propan-2- 10.95-10.86 (m, 1H), 8.81-8.68 m/e459 ylamino)ethyl]amino}-N-[3- (m, 1H), 8.67-8.53 (m, 1H), 8.02- (M +H)⁺ (1H-imidazol-1-yl)propyl]- 7.93 (m, 1H), 7.51 (ddd, J = 5.5,1,3-thiazole-5-carboxamide 4.8, 1.7 Hz, 1H), 7.34 (dd, J = 8.4, 5.5 Hz,2H), 7.14 (s, 1H), 7.07- 6.99 (m, 2H), 5.04 (s, 2H), 4.46 (s, 2H),4.38-4.27 (m, 2H), 3.96 (dd, J = 13.5, 6.8 Hz, 1H), 3.40- 3.27 (m, 2H),2.19-2.17 (m, 2H), 1.18 (d, J = 6.6 Hz, 6H). 20 2-{[2-(dimethylamino)-2-¹H NMR (400 MHz, CDCl₃) δ (ESI(+)) oxoethyl](4- 10.99-10.90 (m, 1H),8.97-8.89 m/e 445 fluorobenzyl)amino}-N-[3- (m, 1H), 8.01 (s, 1H),7.36-7.29 (M + H)⁺ (1H-imidazol-1-yl)propyl]- (m, 2H), 7.22 (t, J = 1.6Hz, 1H), 1,3-thiazole-5-carboxamide 7.13 (t, J = 1.7 Hz, 1H), 7.07- 6.99(m, 2H), 5.36 (s, 2H), 4.45 (s, 2H), 4.41-4.32 (m, 2H), 3.38 (dd, J =11. 1, 5.7 Hz, 2H), 3.12 (s, 3H), 3.00 (s, 3H), 2.23-2.19 (m, 2H). 212-{[2-(diethylamino)-2- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+)) oxoethyl](4-11.08-11.00 (m, 1H), 9.04-8.96 m/e 473 fluorobenzyl)amino}-N-[3- (m,1H), 8.11-8.02 (m, 1H), 7.33 (M + H)⁺ (1H-imidazol-1-yl)propyl]- (dd, J= 8.5, 5.4 Hz, 2H), 7.25 (t, 1,3-thiazole-5-carboxamide J = 1.6 Hz, 1H),7.13 (s, 1H), 7.04 (dd, J = 9.8, 7.5 Hz, 2H), 5.34 (s, 2H), 4.45 (s,2H), 4.36 (dd, J = 7.8, 4.0 Hz, 2H), 3.44-3.37 (m, 6H), 2.24-2.19 (m,2H), 1.29 (t, J = 5.4 Hz, 3H), 1.15 (t, J = 7.1 Hz, 3H). 222-{(4-fluorobenzyl)[2- ¹H NMR (400 MHz, CDCl₃) δ (ESI(+))(morpholin-4-yl)-2- 11.09-11.00 (m, 1H), 8.92-8.79 m/e 487oxoethyl]amino}-N-[3-(1H- (m, 1H), 8.11-8.02 (m, 1H), 7.36- (M + H)⁺imidazol-1-yl)propyl]-1,3- 7.29 (m, 2H), 7.24 (d, J = 1.5thiazole-5-carboxamide Hz, 1H), 7.19-7.11 (m, 1H), 7.06- 6.99 (m, 2H),5.46 (dd, J = 4.8, 2.0 Hz, 2H), 4.45 (d, J = 3.3 Hz, 2H), 4.41-4.30 (m,2H), 3.78 (ddd, J = 6.4, 5.3, 2.4 Hz, 2H), 3.75-3.70 (m, 2H), 3.63-3.57(m, 4H), 3.37 (tdd, J = 7.3, 2.3, 1.4 Hz, 2H), 2.27-2.18 (m, 2H).

Example 262-[(N,N-dimethylglycyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide

Example 6B (0.036 g, 0.1 mmol) was dissolved in dichloromethane:pyridine10:1 (1 ml), cooled to −10° C., and treated with chloroacetyl bromide(0.011 mL, 0.125 mmol). The resultant solution was stirred at roomtemperature for 30 minutes. The reaction mixture was then treated withan excess of dimethylamine in tetrahydrofuran (0.5 mL, 1M solution). Thereaction mixture was heated at 80° C. overnight and purified byreverse-phase HPLC (as described in Example 6C) to afford the titlecompound. ¹H NMR (400 MHz, methanol-d₄) δ 8.98 (s, 1H), 8.03 (s, 1H),7.71 (s, 1H), 7.58 (s, 1H), 7.35-7.23 (m, 2H), 7.10 (t, J=8.7 Hz, 2H),5.48 (s, 2H), 4.60-4.45 (m, 2H), 4.32 (t, J=6.9 Hz, 2H), 3.40 (t, J=6.5Hz, 2H), 2.98 (s, 6H), 2.18 (t, J=6.7 Hz, 2H); MS (ESI(+)) m/e 445(M+H)+.

The following examples were prepared as described in Example 26,substituting the appropriate alkyl halide in Example 26. Title compoundswere purified by either flash chromatography (silica gel column elutingwith a gradient of 0-10% methanol in dichloromethane) or reverse-phaseHPLC (as in described Example 6C). Accordingly, some examples wereisolated as trifluoroacetic acid salts.

EX NAME ¹H NMR DATA MS DATA 27 2-[(3,6-dihydropyridin- ¹H NMR (400 MHz,methanol-d₄) (ESI(+)) 1(2H)-ylacetyl)(4- δ 8.95 (s, 1H), 8.03 (s, 1H),7.69 m/e 483 fluorobenzyl)amino]-N-[3- (s, 1H), 7.56 (s, 1H), 7.28 (s,2H), (M + H)⁺ (1H-imidazol-1-yl)propyl]- 7.10 (t, J = 8.7 Hz, 2H), 5.98(s, 1,3-thiazole-5-carboxamide 1H), 5.73 (s, 1H), 5.51 (s, 2H),4.53-2.44 (m, 2H), 4.32 (t, J = 6.9 Hz, 2H), 3.88-3.78 (m, 1H),3.57-3.42 (m, 1H), 3.40 (t, J = 6.6 Hz, 1H), 2.52-2.46 (m, 2H), 2.17(dd, J = 13.5, 6.8 Hz, 2H). 28 2-{(4-fluorobenzyl)[(4- ¹H NMR (400 MHz,methanol-d₄) (ESI(+)) methylpiperidin-1- δ 8.98 (s, 1H), 8.03 (s, 1H),7.71 m/e 499 yl)acetyl]amino}-N-[3-(1H- (s, 1H), 7.58 (s, 1H), 7.27 (s,2H), (M + H)⁺ imidazol-1-yl)propyl]-1,3- 7.10 (t, J = 8.7 Hz, 2H), 5.49(s, thiazole-5-carboxamide 2H), 4.45 (s, 2H), 4.32 (dd, J = 8.9, 4.9 Hz,2H), 3.63 (d, J = 10.7 Hz, 2H), 3.40 (t, J = 6.5 Hz, 2H), 3.04 (t, J =12.6 Hz, 2H), 2.21- 2.14 (m, 2H), 1.92 (d, J = 15.0 Hz, 2H), 1.71 (s,1H), 1.56 (d, J = 12.4 Hz, 2H), 1.03 (d, J = 6.4 Hz, 3H). 292-{(4-fluorobenzyl)[(4- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))hydroxypiperidin-1- δ 8.98 (s, 1H), 8.03 (s, 1H), 7.71 m/e 501yl)acetyl]amino}-N-[3-(1H- (s, 1H), 7.58 (s, 1H), 7.28 (s, 2H), (M + H)⁺imidazol-1-yl)propyl]-1,3- 7.10 (t, J = 8.7 Hz, 2H), 5.49 (s,thiazole-5-carboxamide 2H), 4.49 (s, 2H), 4.32 (t, J = 7.0 Hz, 2H), 3.46(d, J = 5.3 Hz, 1H), 3.40 (t, J = 6.6 Hz, 2H), 2.19 (dd, J = 13.7, 6.8Hz, 2H), 2.12 (d, J = 22.1 Hz, 2H), 1.91-1.85 (m, 2H). 302-{(4-fluorobenzyl)[(4- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))methylpiperazin-1- δ 8.99 (s, 1H), 7.99 (s, 1H), 7.71 m/e 500yl)acetyl]amino}-N-[3-(1H- (d, J = 1.4 Hz, 1H), 7.59 (s, 1H), (M + H)⁺imidazol-1-yl)propyl]-1,3- 7.27-7.15 (m, 2H), 7.08 (t, J =thiazole-5-carboxamide 8.7 Hz, 2H), 5.54 (s, 2H), 4.33 (t, J = 7.0 Hz,2H), 3.71 (s, 2H), 3.40 (t, J = 6.5 Hz, 2H), 3.13-2.91 (m, 4H), 2.88 (s,3H), 2.82-2.66 (m, 2H), 2.19 (p, J = 7.0 Hz, 2H). 312-[(4-fluorobenzyl){[4- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))(propan-2-yl)piperazin-1- δ 8.99 (s, 1H), 7.99 (s, 1H), 7.72 m/e 528yl]acetyl}amino]-N-[3-(1H- (t, J = 1.6 Hz, 1H), 7.59 (t, J = 1.6 (M +H)⁺ imidazol-1-yl)propyl]-1,3- Hz, 1H), 7.21 (dd, J = 8.6, 5.3 Hz,thiazole-5-carboxamide 2H), 7.08 (dd, J = 12.2, 5.3 Hz, 2H), 5.55 (s,2H), 4.33 (t, J = 6.9 Hz, 2H), 3.71 (s, 2H), 3.51-3.37 (m, 4H),3.15-2.91 (m, 4H), 2.75- 2.67 (m, 1H), 2.19 (t, J = 6.7 Hz, 2H), 1.33(d, J = 6.7 Hz, 6H). 32 2-{(4-fluorobenzyl)[(4- ¹H NMR (400 MHz,methanol-d₄) (ESI(+)) formylpiperazin-1- δ 8.99 (s, 1H), 8.05 (s, 1H),8.00 m/e 514 yl)acetyl]amino}-N-[3-(1H- (d, J = 9.0 Hz, 1H), 7.72 (s,1H), (M + H)⁺ imidazol-1-yl)propyl]-1,3- 7.59 (s, 1H), 7.31-7.19 (m,2H), thiazole-5-carboxamide 7.15-7.03 (m, 2H), 5.66-5.41 (m, 2H), 4.33(t, J = 7.0 Hz, 2H), 4.21-4.03 (m, 2H), 3.68 (tdd, J = 5.0, 4.5, 1.3 Hz,2H), 3.66-3.60 (m, 2H), 3.46-3.38 (m, 2H), 3.16- 2.93 (m, 4H), 2.25-2.13(m, 2H). 33 2-[(4- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))fluorobenzyl)(hexahydropyr- δ 8.99 (s, 1H), 7.99 (s, 1H), 7.72 m/e 526rolo[1,2-a]pyrazin-2(1H)- (t, J = 1.6 Hz, 1H), 7.59 (t, J = 1.5 (M + H)⁺ylacetyl)amino]-N-[3-(1H- Hz, 1H), 7.21 (dd, J = 8.5, 5.3 Hz,imidazol-1-yl)propyl]-1,3- 2H), 7.08 (t, J = 8.7 Hz, 2H), 5.54thiazole-5-carboxamide (s, 2H), 4.33 (t, J = 6.9 Hz, 2H), 3.81-3.68 (m,2H), 3.39 (d, J = 6.5 Hz, 2H), 3.26-2.68 (m, 6H), 2.28-2.01 (m, 5H). 342-[{[4- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))(cyclopropylmethyl)piperazin- δ 8.99 (s, 1H), 8.00 (s, 1H), 7.72 m/e 5401-yl]acetyl}(4- (t, J = 1.7 Hz, 1H), 7.59 (s, 1H), (M + H)⁺fluorobenzyl)amino]-N-[3- 7.27-7.15 (m, 2H), 7.15-7.02(1H-imidazol-1-yl)propyl]- (m, 2H), 5.55 (s, 2H), 4.33 (t, J =1,3-thiazole-5-carboxamide 6.9 Hz, 2H), 3.72 (s, 2H), 3.65- 3.50 (m,2H), 3.40 (dd, J = 8.0, 5.1 Hz, 2H), 3.17-2.97 (m, 6H), 2.88-2.68 (m,2H), 2.26-2.11 (m, 2H), 1.06 (d, J = 7.2 Hz, 1H), 0.83-0.70 (m, 2H),0.43 (dd, J = 5.6, 4.9 Hz, 2H). 35 2-[{[4-(2- ¹H NMR (400 MHz,methanol-d₄) (ESI(+)) ethoxyethyl)piperazin-1- δ 8.99 (s, 1H), 7.99 (s,1H), 7.72 m/e 558 yl]acetyl}(4- (s, 1H), 7.59 (s, 1H), 7.21 (dd, J =(M + H)⁺ fluorobenzyl)amino]-N-[3- 8.6, 5.2 Hz, 2H), 7.09-7.06 (m,(1H-imidazol-1-yl)propyl]- 2H), 5.55 (s, 2H), 4.39-4.24 (m,1,3-thiazole-5-carboxamide 2H), 3.74 (dd, J = 6.4, 3.6 Hz, 2H), 3.71 (s,2H), 3.57 (q, J = 7.1 Hz, 2H), 3.40 (t, J = 6.5 Hz, 2H), 2.95 (d, J =58.3 Hz, 6H), 2.26- 2.09 (m, 2H), 1.22 (t, J = 7.0 Hz, 3H). 372-[(4-fluorobenzyl){[4- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))(prop-2-en-1-yl)piperazin-1- δ 8.99 (s, 1H), 8.00 (s, 1H), 7.71 m/e 526yl]acetyl}amino]-N-[3-(1H- (d, J = 7.5 Hz, 1H), 7.58 (s, 1H), (M + H)+imidazol-1-yl)propyl]-1,3- 7.21 (dd, J = 8.5, 5.3 Hz, 2H),thiazole-5-carboxamide 7.08 (t, J = 8.7 Hz, 2H), 6.01- 5.82 (m, 1H),5.62 (s, 1H), 5.59 (d, J = 6.2 Hz, 1H), 5.54 (s, 2H), 4.33 (t, J = 6.9Hz, 2H), 3.74 (d, J = 7.3 Hz, 2H), 3.75-3.70 (m, 2H), 3.40 (t, J = 6.5Hz, 2H), 2.95- 2.9 (m, 4H), 2.19 (p, J = 6.9 Hz, 2H). 382-[(4-fluorobenzyl){[4-(3- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))methoxypropyl)piperazin-1- δ 8.99 (s, 1H), 8.00 (s, 1H), 7.71 m/e 558yl]acetyl}amino]-N-[3-(1H- (s, 1H), 7.58 (s, 1H), 7.21 (dd, J = (M + H)+imidazol-1-yl)propyl]-1,3- 8.5, 5.3 Hz, 2H), 7.08 (t, J = 8.7thiazole-5-carboxamide Hz, 2H), 5.55 (s, 2H), 4.33 (t, J = 6.9 Hz, 2H),3.71 (s, 2H), 3.48 (t, J = 5.6 Hz, 2H), 3.40 (t, J = 6.5 Hz, 2H), 3.34(s, 3H), 3.23 (t, J = 8.0 Hz, 2H), 2.26-2.09 (m, 2H), 1.97 (dd, J = 9.7,5.8 Hz, 2H). 39 2-[{[3- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))(dimethylamino)pyrrolidin- δ 8.99 (s, 1H), 8.01 (s, 1H), 7.71 m/e 5141-yl]acetyl}(4- (s, 1H), 7.58 (s, 1H), 7.24 (dd, J = (M + H)+fluorobenzyl)amino]-N-[3- 8.5, 5.3 Hz, 2H), 7.08 (t, J = 8.7(1H-imidazol-1-yl)propyl]- Hz, 2H), 5.51 (s, 2H), 4.33 (t, J =1,3-thiazole-5-carboxamide 6.9 Hz, 2H), 4.06 (d, J = 32.5 Hz, 2H),3.97-3.90 (m, 1H), 3.52- 3.43 (m, 1H), 3.40 (t, J = 6.5 Hz, 2H), 3.13(s, 1H), 2.91 (s, 6H), 2.40 (dd, J = 13. 1, 4.6 Hz, 1H), 2.26-2.06 (m,3H). 40 2-[(4- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))fluorobenzyl)(morpholin-4- δ 8.99 (s, 1H), 8.04 (s, 1H), 7.71 m/e 487ylacetyl)amino]-N-[3-(1H- (s, 1H), 7.58 (s, 1H), 7.35-7.23 (M + H)+imidazol-1-yl)propyl]-1,3- (m, 2H), 7. 1 0 (t, J = 8.7 Hz, 2H),thiazole-5-carboxamide 5.50 (s, 2H), 4.54 (s, 2H), 4.33 (t, J = 6.9 Hz,2H), 3.99-3.90 (m, 4H), 3.53-3.33 (m, 6H), 2.19 (p, J = 6.8 Hz, 2H). 412-{(4-fluorobenzyl)[(3- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))hydroxypiperidin-1- δ 8.99 (s, 1H), 8.04 (s, 1H), 7.71 m/e 501yl)acetyl]amino}-N-[3-(1H- (s, 1H), 7.59 (s, 1H), 7.34-7.23 (M + H)+imidazol-1-yl)propyl]-1,3- (m, 2H), 7. 1 0 (t, J = 8.7 Hz, 2H),thiazole-5-carboxamide 5.50 (s, 2H), 4.50 (m, 1H), 4.33 (t, J = 7.0 Hz,2H), 4.15-4.1 (m, 1H), 3.76-3.49 (m, 1H), 3.40 (t, J = 6.6 Hz, 2H),3.27-2.95 (m, 2H), 2.19 (p, J = 6.8 Hz, 2H), 1.79 (d, J = 15.5 Hz, 2H).42 2-[(4-fluorobenzyl){[4-(2- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))hydroxyethyl)piperazin-1- δ 8.99 (s, 1H), 8.00 (s, 1H), 7.72 m/e 530yl]acetyl}amino]-N-[3-(1H- (s, 1H), 7.58 (s, 1H), 7.22 (dd, J = (M + H)+imidazol-1-yl)propyl]-1,3- 8.6, 5.3 Hz, 2H), 7.08 (t, J = 8.7thiazole-5-carboxamide Hz, 2H), 5.55 (s, 2H), 4.33 (t, J = 6.9 Hz, 2H),3.91-3.80 (m, 2H), 3.75-3.65 (m, 2H), 3.40 (t, J = 6.5 Hz, 2H),3.26-3.21 (m, 2H), 2.98-2.88 (m, 4H), 2.19 (p, J = 6.7 Hz, 2H). 432-[(1,4-dioxa-7- ¹H NMR (400 MHz, methanol-d₄) (ESI(+))azaspiro[4.4]non-7- δ 8.99 (s, 1H), 8.03 (s, 1H), 7.71 m/e 529ylacetyl)(4- (s, 1H), 7.58 (s, 1H), 7.35-7.23 (M + H)+fluorobenzyl)amino]-N-[3- (m, 2H), 7. 1 0 (t, J = 8.7 Hz, 2H),(1H-imidazol-1-yl)propyl]- 5.48 (s, 2H), 4.64 (s, 2H), 4.33 (t,1,3-thiazole-5-carboxamide J = 6.9 Hz, 2H), 3.99 (d, J = 3.7 Hz, 4H),3.72-3.63 (m, 2H), 3.6- 3.5 (m, 2H), 3.40 (t, J = 6.5 Hz, 2H), 2.29 (t,J = 7.7 Hz, 2H), 2.19 (p, J = 6.7 Hz, 2H).

Example 2122-{(5S)-5-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-2-oxo-1,3-oxazolidin-3-yl}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide

Example 6A (0.095 g, 0.3 mmol),(R)-2-((2-oxooxazolidin-5-yl)methyl)isoindoline-1,3-dione (0.049 g, 0.2mmol), and potassium phosphate (0.127 g, 0.6 mmol) were suspended in drydioxane, and nitrogen was bubbled through for 5 minutes.Tris(dibenzylideneacetone)dipalladium(0) (0.018 g. 0.02 mmol) and4,5-bis(diphenylphosphino)-9,9-dimethylxanthene (XantPhos, 0.035 g, 0.06mmol) were added to the reaction, and the vial capped. The reaction wasstirred at 90° C. for 5 hours, concentrated and submitted to reversephase HPLC (as described in Example 6C) to afford the title compound. ¹HNMR (400 MHz, methanol-d₄) δ 8.98 (s, 1H), 7.95 (s, 1H), 7.90 (dt,J=7.3, 3.7 Hz, 2H), 7.87-7.80 (m, 2H), 7.71 (d, J=1.6 Hz, 1H), 7.58 (t,J=1.6 Hz, 1H), 5.16 (dt, J=12.7, 5.8 Hz, 1H), 4.40 (dd, J=10.2, 8.8 Hz,1H), 4.33 (t, J=6.8 Hz, 2H), 4.20 (dd, J=10.4, 5.8 Hz, 1H), 4.10 (ddd,J=19.6, 14.6, 5.9 Hz, 2H), 3.39 (dd, J=11.2, 6.1 Hz, 2H), 2.18 (p, J=6.7Hz, 2H); MS (ESI(+)) m/e 480.5 (M+H)+.

The following examples were prepared as described in Example 212,substituting the appropriate imidazolidinone for the oxazolidinone.Title compounds were purified by either flash chromatography (silica gelcolumn eluting with a gradient of 0-10% methanol in dichloromethane) orreverse-phase HPLC (as described in Example 6C). Accordingly, someexamples were isolated as trifluoroacetic acid salts.

EX NAME ¹H NMR DATA MS DATA 203 2-[3-(2-hydroxyethyl)-2- ¹H NMR (400MHz, methanol-d₄) (ESI(+)) oxoimidazolidin-1-yl]-N-[3- δ 7.89 (s, 1H),7.70 (s, 1H), 7.18 m/e 365 (1H-imidazol-1-yl)propyl]- (s, 1H), 6.97 (s,1H), 4.10 (dd, J = (M + H)⁺ 1,3-thiazole-5-carboxamide 11.6, 4.7 Hz,4H), 3.74 (dd, J = 12.9, 7.2 Hz, 4H), 3.43 (t, J = 5.4 Hz, 2H), 3.34 (t,J = 6.8 Hz, 2H), 2.07 (p, J = 6.8 Hz, 2H). 204 2-[3-(4-fluorophenyl)-2-¹H NMR (400 MHz, methanol-d₄) (ESI(+)) oxoimidazolidin-1-yl]-N-[3- δ8.99 (s, 1H), 7.95 (s, 1H), 7.76- m/e 415 (1H-imidazol-1-yl)propyl]-7.54 (m, 4H), 7.15 (t, J = 8.8 Hz, (M + H)⁺ 1,3-thiazole-5-carboxamide2H), 4.34 (t, J = 6.8 Hz, 2H), 4.24 (dd, J = 10.0, 6.5 Hz, 2H), 4.13(dd, J = 9.9, 6.7 Hz, 2H), 3.40 (dd, J = 11.5, 6.0 Hz, 2H), 2.19 (p, J =6.6 Hz, 2H).

What is claimed is:
 1. A compound of formula (I), or a therapeuticallyacceptable salt thereof,

wherein R¹ and R² are each independently selected from the groupconsisting of R⁶, C(O)R⁶, C(O)NHR⁶, and C(O)N(R⁶)₂; wherein at least oneof R¹ and R² is R⁶; or R¹ and R², together with the nitrogen to whichthey are attached form a heterocycloalkyl or heterocycloalkenyl ring;wherein the ring formed with R¹ and R² together with the nitrogen towhich they are attached is optionally substituted with one or moresubstituents independently selected from the group consisting of R⁷,OR⁷, SR⁷, S(O)R⁷, SO₂R⁷, C(O)R⁷, CO(O)R⁷, OC(O)R⁷, OC(O)OR⁷, NH₂, NHR⁷,N(R⁷)₂, NHC(O)R⁷, NR⁷C(O)R⁷, NHS(O)₂R⁷, NR⁷S(O)₂R⁷, NHC(O)OR⁷,NR⁷C(O)OR⁷, NHC(O)NH₂, NHC(O)NHR⁷, NHC(O)N(R⁷)₂, NR⁷C(O)NHR⁷,NR⁷C(O)N(R⁷)₂, C(O)NH₂, C(O)NHR⁷, C(O)N(R⁷)₂, C(O)NHOH, C(O)NHOR⁷,C(O)NHSO₂R⁷, C(O)NR⁷SO₂R⁷, SO₂NH₂, SO₂NHR⁷, SO₂N(R⁷)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁷, C(N)N(R⁷)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; R³, R⁴, and R⁵ are each independently selected from the groupconsisting of hydrogen, C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆haloalkyl, C₁₋₆ hydroxyalkyl, F, Cl, Br and I; R⁶, at each occurrence,is independently selected from the group consisting of C₁₋₆ alkyl, C₂₋₆alkenyl, C₂₋₆ alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R⁶ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of R⁸, OR⁸, SR⁸, S(O)R⁸, SO₂R⁸,C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂, NHR⁸, N(R⁸)₂, NHC(O)R⁸,NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸, NR⁸C(O)OR⁸, NHC(O)NH₂,NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸, NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸,C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸, C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂,SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR⁸, C(N)N(R⁸)₂, CNOH,CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁶ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R⁹, OR⁹, SR⁹, S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹,OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂, NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹,NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹, NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂,NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂, C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH,C(O)NHOR⁹, C(O)NHSO₂R⁹, C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H,C(O)OH, C(N)NH₂, C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F,Cl, Br and I; R⁷, at each occurrence, is independently selected from thegroup consisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁷ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofaryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl,cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I;wherein the aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl represented by R⁷ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I; R⁸, at each occurrence, is independently selectedfrom the group consisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl,aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁸ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰,OC(O)OR¹⁰, NH₂, NHR¹⁰, N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰,NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰, NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰,NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰, NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰,C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰, C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂,SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂,CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁸ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹, C(O)R¹¹,CO(O)R¹¹, OC(O)R¹¹, OC(O)OR¹¹, NH₂, NHR¹¹, N(R¹¹)₂, NHC(O)R¹¹,NR¹¹C(O)R¹¹, NHS(O)₂R¹¹, NR¹¹S(O)₂R¹¹, NHC(O)OR¹¹, NR¹¹C(O)OR¹¹,NHC(O)NH₂, NHC(O)NHR¹¹, NHC(O)N(R¹¹)₂, NR¹¹C(O)NHR¹¹, NR¹¹C(O)N(R¹¹)₂,C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)NHOH, C(O)NHOR¹¹, C(O)NHSO₂R¹¹,C(O)NR¹¹SO₂R¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹¹, C(N)N(R¹¹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;R⁹, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁹ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹², OR¹², SR¹², S(O)R¹², SO₂R¹², C(O)R¹², CO(O)R¹², OC(O)R¹²,OC(O)OR¹², NH₂, NHR¹², N(R¹²)₂, NHC(O)R¹², NR¹²C(O)R¹², NHS(O)₂R¹²,NR¹²S(O)₂R¹², NHC(O)OR¹², NR¹²C(O)OR¹², NHC(O)NH₂, NHC(O)NHR¹²,NHC(O)N(R¹²)₂, NR¹²C(O)NHR¹², NR¹²C(O)N(R¹²)₂, C(O)NH₂, C(O)NHR¹²,C(O)N(R¹²)₂, C(O)NHOH, C(O)NHOR¹², C(O)NHSO₂R¹², C(O)NR¹²SO₂R¹², SO₂NH₂,SO₂NHR¹², SO₂N(R¹²)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR¹², C(N)N(R¹²)₂,CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁹ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³,CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³,NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³,NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂,C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³,C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹³, C(N)N(R¹³)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;R¹⁰ at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl,and C₁₋₆ hydroxyalkyl; R¹¹, at each occurrence, is independentlyselected from the group consisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, andC₂₋₆ alkynyl represented by R¹¹ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of C₁₋₆ alkoxy, aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, cycloalkenyl, NH₂, C(O)H,C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R¹¹ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Brand I; R¹², at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R¹² are each independently optionally substituted withone or more substituents independently selected from the groupconsisting of C₁₋₆ alkoxy, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I; wherein the aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl representedby R¹² are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of NH₂,C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I; and R¹³, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R¹³ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of alkoxy, NH₂, C(O)H, C(O)OH, OH,CN, N₃, NO₂, F, Cl, Br and I.
 2. The compound of claim 1, wherein R¹ isC(O)R⁶; and R² is R⁶.
 3. The compound of claim 1, wherein R¹ and R² areeach R⁶.
 4. The compound of claim 1, wherein R¹ is C(O)NHR⁶; and R² isR⁶.
 5. The compound of claim 1, wherein R¹ is C(O)N(R⁶)₂; and R² is R⁶.6. The compound of any one of claims 1-5, wherein R³, R⁴, and R⁵ arehydrogen.
 7. The compound of any one of claims 1-5, wherein R⁶, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl, C₂₋₆ alkenyl, aryl, heterocycloalkyl, heteroaryl, and cycloalkyl;wherein the C₁₋₆ alkyl, and C₂₋₆ alkenyl represented by R⁶ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁸, OR⁸, C(O)R⁸,CO(O)R⁸, OC(O)R⁸, N(R⁸)₂, NHC(O)R⁸, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂,C(O)OH, and OH; wherein the aryl, heterocycloalkyl, heteroaryl, andcycloalkyl represented by R⁶ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R⁹, OR⁹, C(O)NH₂, C(O)OH, OH, CN, F, Cl, Br andI.
 8. The compound of claim 1, selected from the group consisting of:2-{(4-fluorobenzyl)[4-(pyridin-3-yl)benzyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{methyl[4-(pyridin-3-yl)benzyl]amino}-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl)(methyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl)(tetrahydro-2H-pyran-4-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(cyclohexylacetyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl)(3-methylbutanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[3-(morpholin-4-yl)propyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[3-(piperidin-1-yl)propyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[2-(pyrrolidin-1-yl)ethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl){2-[4-(propan-2-yl)piperazin-1-yl]ethyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzoyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(3-chlorobenzoyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzoyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[(5-chloro-1,3-benzodioxol-4-yl)methyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-chlorobenzyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(2-chlorobenzyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(2,5-dichlorobenzyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[2-(methylamino)-2-oxoethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[2-oxo-2-(propan-2-ylamino)ethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[2-(dimethylamino)-2-oxoethyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[2-(diethylamino)-2-oxoethyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[2-(morpholin-4-yl)-2-oxoethyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl)(4-methylbenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl)(methoxyacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(N,N-dimethylglycyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(3,6-dihydropyridin-1(2H)-ylacetyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(4-methylpiperidin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(4-hydroxypiperidin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(4-methylpiperazin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl){[4-(propan-2-yl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(4-formylpiperazin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl)(hexahydropyrrolo[1,2-a]pyrazin-2(1H)-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[{[4-(cyclopropylmethyl)piperazin-1-yl]acetyl}(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[{[4-(2-ethoxyethyl)piperazin-1-yl]acetyl}(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(cyclopropylcarbonyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl){[4-(prop-2-en-1-yl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl){[4-(3-methoxypropyl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[{[3-(dimethylamino)pyrrolidin-1-yl]acetyl}(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl)(morpholin-4-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(3-hydroxypiperidin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl){[4-(2-hydroxyethyl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(1,4-dioxa-7-azaspiro[4.4]non-7-ylacetyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;1-{2-[(4-fluorobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)amino]-2-oxoethyl}pyridinium;2-{[2-(4-fluorophenyl)ethyl](3-methylbutanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl)(propan-2-ylcarbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[2-(4-cyanophenyl)ethyl](3-methylbutanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[2-(4-cyanophenyl)ethyl](tetrahydro-2H-pyran-4-ylacetyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzyl)(3-methylbutanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzyl)(tetrahydro-2H-pyran-4-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[2-(4-cyanophenyl)ethyl](tetrahydrofuran-3-ylacetyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl)(3-methylbutanoyl)amino]-N-[3-(2-methyl-1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl)(3-methylbutanoyl)amino]-N-[3-(4-methyl-1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(2-fluorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(3-fluorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(2-chlorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(3-chlorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-chlorobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzyl)(tetrahydrofuran-3-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(3-methylbutyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(2-methylpropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N¹-(4-fluorobenzyl)-N¹-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)piperidine-1,3-dicarboxamide;2-{(4-fluorobenzyl)[(3-hydroxyazetidin-1-yl)carbonyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-1,4-dioxa-7-azaspiro[4.4]nonane-7-carboxamide;2-{(4-fluorobenzyl)[(3-methoxypyrrolidin-1-yl)carbonyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(2-methoxyethyl)(methyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-2,6-dimethylmorpholine-4-carboxamide;2-{[ethyl(2-methoxyethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-2,2-dimethylmorpholine-4-carboxamide;N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-1,4-oxazepane-4-carboxamide;2-[(4-fluorobenzoyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(4-methylbenzyl)amino]-1,3-thiazole-5-carboxamide;N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-N-(3-methylbutyl)-1,2-oxazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(2-phenoxypropanoyl)amino]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(2-propoxyethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(tetrahydrofuran-2-ylmethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(1-methoxypropan-2-yl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(tetrahydro-2H-pyran-2-ylmethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(2-methoxyethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[(2-ethoxyethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(1-methoxybutan-2-yl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[2-(4-cyanophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[(1,3-dioxolan-2-ylmethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl){[2-(propan-2-yloxy)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[(1,4-dioxan-2-ylmethyl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[(1,3-dimethoxypropan-2-yl)carbamoyl](4-fluorobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(2-methoxybutyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl)(tetrahydrofuran-3-ylcarbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl)(tetrahydro-2H-pyran-3-ylcarbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(pyrimidin-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(2-methoxypyridin-4-yl)methyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(1,3-oxazol-4-ylmethyl)amino]-1,3-thiazole-5-carboxamide;2-{[(5-chloropyridin-2-yl)methyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(4-methylpyridin-3-yl)methyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(6-methoxypyridin-3-yl)methyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(4-methyl-1,3-thiazol-5-yl)methyl]amino}-1,3-thiazole-5-carboxamide;2-{[2-(3-hydroxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(pyridin-2-ylethyl]amino}-1,3-thiazole-5-carboxamideacetate (1:1);2-{[2-(1,3-benzodioxol-5-yl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamideacetate (1:1);2-{[2-(4-chlorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamideacetate (1:1);2-{[2-(3-fluorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamideacetate (1:1);2-{[2-(4-hydroxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamideacetate (1:1);2-{[2-(3-chlorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamideacetate (1:1);N-[3-(1H-imidazol-1-yl)propyl]-2-{[2-(3-methoxyphenyl)ethyl](3-methoxypropanoyl)amino}-1,3-thiazole-5-carboxamideacetate (1:1);2-{[2-(2-fluorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamideacetate (1:1);2-{[2-hydroxy-2-(4-methoxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamideacetate (1:1);N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[1-(pyridin-2-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(1-methyl-1H-pyrazol-4-yl)methyl]amino}-1,3-thiazole-5-carboxamide;2-[(2,6-difluorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(6-methylpyridin-3-yl)methyl]amino}-1,3-thiazole-5-carboxamide;2-[(4-chlorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(5-methylpyrazin-2-yl)methyl]amino}-1,3-thiazole-5-carboxamide;2-[(3-chlorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(5-methylpyridin-2-yl)methyl]amino}-1,3-thiazole-5-carboxamide;2-[(2,5-difluorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(2-methylbenzyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(3-methylbenzyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(pyridin-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(pyridin-3-ylmethyl)amino]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzyl){[2-(propan-2-yloxy)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-cyanobenzyl)[(2-methoxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzyl){[2-(2-hydroxyethoxy)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzyl){[3-(propan-2-yloxy)propyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-cyanobenzyl)[(3-hydroxy-2,2-dimethylpropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-cyanobenzyl)[(2-hydroxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-cyanobenzyl)[(1-hydroxypropan-2-yl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-cyanobenzyl)[(3-hydroxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzyl){[(2S)-1-hydroxybut-3-en-2-yl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-cyanobenzyl)[(4-hydroxybutyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methylbutyl)[(2R)-2-phenoxypropanoyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methylbutyl)[(2S)-2-phenoxypropanoyl]amino}-1,3-thiazole-5-carboxamide;N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-5-methyl-N-(3-methylbutyl)-1,2-oxazole-3-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(phenoxyacetyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(3-phenylpropanoyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(2-phenylpropanoyl)amino]-1,3-thiazole-5-carboxamide;2-{[(4-fluorophenyl)acetyl](3-methylbutyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[(3-amino-3-oxopropyl)carbamoyl](4-cyanobenzyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[{[3-(acetylamino)-2-methylpropyl]carbamoyl}(4-cyanobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzyl){[3-(dimethylamino)-3-oxopropyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-cyanobenzyl)[(3-ethoxy-2-hydroxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzyl){[3-(diethylamino)propyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[{[2-(acetylamino)ethyl]carbamoyl}(4-cyanobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzyl){[2-(diethylamino)ethyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzyl)({2-[(2-methylpropanoyl)amino]ethyl}carbamoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzyl){[(2R)-1-hydroxybut-3-en-2-yl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzyl){[3-(3-hydroxyazetidin-1-yl)propyl]carbamoyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(3-methylbutyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(methoxyacetyl)(3-methylbutyl)amino]-1,3-thiazole-5-carboxamide;2-[(cyclopropylcarbonyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;(2S)-1-[(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)(3-methylbutyl)amino]-1-oxopropan-2-ylacetate;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydro-2H-pyran-4-ylacetyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydrofuran-3-ylcarbonyl)amino]-1,3-thiazole-5-carboxamide;2-{[2-hydroxy-2-(3-methoxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(pyrazin-2-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;2-{[1-(3-hydroxyphenyl)propan-2-yl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;ethylN-[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]-beta-alaninate;ethyl4-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoate;ethyl3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoate;ethyl3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-4-methylpentanoate;ethyl3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2,2-dimethylpropanoate;3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}cyclobutanecarboxylicacid; ethyl3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2-methylpropanoate;2-{(4-cyanobenzyl)[(3-methoxypropyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoicacid;3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-4-methylpentanoicacid;3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2,2-dimethylpropanoicacid;3-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}-2-methylpropanoicacid;N-[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]-beta-alanine;4-{[(4-cyanobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)carbamoyl]amino}butanoicacid;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydrofuran-2-ylacetyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydrofuran-3-ylacetyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(3-methoxypropanoyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(3-methoxypropyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(tetrahydro-2H-pyran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(tetrahydrofuran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(propan-2-yloxy)ethyl]amino}-1,3-thiazole-5-carboxamide;2-{[2-(1,3-dioxolan-2-yl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(1,4-dioxan-2-ylmethyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[3-(4-fluorophenyl)propanoyl](2-methoxyethyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(2-methoxyethyl)[3-(pyridin-3-yl)propanoyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(pyridin-3-ylacetyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(naphthalen-2-ylacetyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(2-methoxyethyl)[(4-phenoxyphenyl)acetyl]amino}-1,3-thiazole-5-carboxamide;2-{[(4-cyanophenyl)acetyl](2-methoxyethyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[(4-aminophenyl)acetyl](2-methoxyethyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[{2-[di(prop-2-en-1-yl)amino]ethyl}(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[3-(diethylamino)propyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[2-(diethylamino)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-(pyrrolidin-1-yl)propyl]amino}-1,3-thiazole-5-carboxamide;2-{[(1-ethyl-5-oxopyrrolidin-3-yl)methyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(5-oxopyrrolidin-2-yl)methyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-oxo-3-(pyrrolidin-1-yl)propyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-oxo-2-(piperidin-1-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-(2-oxopyrrolidin-1-yl)propyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(2-oxo-1,3-oxazolidin-3-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl){2-[(2-methylpropanoyl)amino]ethyl}amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-(methylamino)-3-oxopropyl]amino}-1,3-thiazole-5-carboxamide;2-{[3-(acetylamino)propyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-oxo-2-(pyrrolidin-1-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;2-[3-(2-hydroxyethyl)-2-oxoimidazolidin-1-yl]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[3-(4-fluorophenyl)-2-oxoimidazolidin-1-yl]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[(5-chloropyridin-2-yl)methyl](tetrahydro-2H-pyran-4-ylcarbonyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[(5-chloropyridin-2-yl)methyl](tetrahydrofuran-3-ylcarbonyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[2-(5-chloropyridin-2-yl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[2-(5-chloropyridin-2-yl)ethyl](tetrahydrofuran-3-ylcarbonyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[2-(5-chloropyridin-2-yl)ethyl][(2-methoxyethyl)carbamoyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-([2-(5-chloropyridin-2-yl)ethyl]{[2-(propan-2-yloxy)ethyl]carbamoyl}amino)-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(1,3-benzodioxol-5-ylacetyl)(2-methoxyethyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(5S)-5-[(1,3-dioxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-2-oxo-1,3-oxazolidin-3-yl}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(pyridin-2-ylacetyl)amino]-1,3-thiazole-5-carboxamide;and pharmaceutically acceptable salts thereof.
 9. A compositioncomprising an excipient and a therapeutically effective amount of acompound of claim 1, or pharmaceutically acceptable salts thereof.
 10. Acompound of claim 1 of formula (III), or a pharmaceutically acceptablesalt thereof,

wherein R⁶, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁶ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR⁸, OR⁸, SR⁸, S(O)R⁸, SO₂R⁸, C(O)R⁸, CO(O)R⁸, OC(O)R⁸, OC(O)OR⁸, NH₂,NHR⁸, N(R⁸)₂, NHC(O)R⁸, NR⁸C(O)R⁸, NHS(O)₂R⁸, NR⁸S(O)₂R⁸, NHC(O)OR⁸,NR⁸C(O)OR⁸, NHC(O)NH₂, NHC(O)NHR⁸, NHC(O)N(R⁸)₂, NR⁸C(O)NHR⁸,NR⁸C(O)N(R⁸)₂, C(O)NH₂, C(O)NHR⁸, C(O)N(R⁸)₂, C(O)NHOH, C(O)NHOR⁸,C(O)NHSO₂R⁸, C(O)NR⁸SO₂R⁸, SO₂NH₂, SO₂NHR⁸, SO₂N(R⁸)₂, C(O)H, C(O)OH,C(N)NH₂, C(N)NHR⁸, C(N)N(R⁸)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Brand I; wherein the aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, and cycloalkenyl represented by R⁶ are eachindependently optionally substituted with one or more substituentsindependently selected from the group consisting of R⁹, OR⁹, SR⁹,S(O)R⁹, SO₂R⁹, C(O)R⁹, CO(O)R⁹, OC(O)R⁹, OC(O)OR⁹, NH₂, NHR⁹, N(R⁹)₂,NHC(O)R⁹, NR⁹C(O)R⁹, NHS(O)₂R⁹, NR⁹S(O)₂R⁹, NHC(O)OR⁹, NR⁹C(O)OR⁹,NHC(O)NH₂, NHC(O)NHR⁹, NHC(O)N(R⁹)₂, NR⁹C(O)NHR⁹, NR⁹C(O)N(R⁹)₂,C(O)NH₂, C(O)NHR⁹, C(O)N(R⁹)₂, C(O)NHOH, C(O)NHOR⁹, C(O)NHSO₂R⁹,C(O)NR⁹SO₂R⁹, SO₂NH₂, SO₂NHR⁹, SO₂N(R⁹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR⁹, C(N)N(R⁹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;R⁸, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁸ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹⁰, OR¹⁰, SR¹⁰, S(O)R¹⁰, SO₂R¹⁰, C(O)R¹⁰, CO(O)R¹⁰, OC(O)R¹⁰,OC(O)OR¹⁰, NH₂, NHR¹⁰, N(R¹⁰)₂, NHC(O)R¹⁰, NR¹⁰C(O)R¹⁰, NHS(O)₂R¹⁰,NR¹⁰S(O)₂R¹⁰, NHC(O)OR¹⁰, NR¹⁰C(O)OR¹⁰, NHC(O)NH₂, NHC(O)NHR¹⁰,NHC(O)N(R¹⁰)₂, NR¹⁰C(O)NHR¹⁰, NR¹⁰C(O)N(R¹⁰)₂, C(O)NH₂, C(O)NHR¹⁰,C(O)N(R¹⁰)₂, C(O)NHOH, C(O)NHOR¹⁰, C(O)NHSO₂R¹⁰, C(O)NR¹⁰SO₂R¹⁰, SO₂NH₂,SO₂NHR¹⁰, SO₂N(R¹⁰)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR¹⁰, C(N)N(R¹⁰)₂,CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁸ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹¹, OR¹¹, SR¹¹, S(O)R¹¹, SO₂R¹¹, C(O)R¹¹,CO(O)R¹¹, OC(O)R¹¹, OC(O)OR¹¹, NH₂, NHR¹¹, N(R¹)₂, NHC(O)R¹¹,NR¹¹C(O)R¹¹, NHS(O)₂R¹¹, NR¹¹S(O)₂R¹¹, NHC(O)OR¹¹, NR¹¹C(O)OR¹¹,NHC(O)NH₂, NHC(O)NHR¹¹, NHC(O)N(R¹¹)₂, NR¹¹C(O)NHR¹¹, NR¹¹C(O)N(R¹¹)₂,C(O)NH₂, C(O)NHR¹¹, C(O)N(R¹¹)₂, C(O)NHOH, C(O)NHOR¹¹, C(O)NHSO₂R¹¹,C(O)NR¹¹SO₂R¹¹, SO₂NH₂, SO₂NHR¹¹, SO₂N(R¹¹)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹¹, C(N)N(R¹¹)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;R⁹, at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R⁹ are each independently optionally substituted with oneor more substituents independently selected from the group consisting ofR¹², OR¹², SR¹², S(O)R¹², SO₂R¹², C(O)R¹², CO(O)R¹², OC(O)R¹²,OC(O)OR¹², NH₂, NHR¹², N(R¹²)₂, NHC(O)R¹², NR¹²C(O)R¹², NHS(O)₂R¹²,NR¹²S(O)₂R¹², NHC(O)OR¹², NR¹²C(O)OR¹², NHC(O)NH₂, NHC(O)NHR¹²,NHC(O)N(R¹²)₂, NR¹²C(O)NHR¹², NR¹²C(O)N(R¹²)₂, C(O)NH₂, C(O)NHR¹²,C(O)N(R¹²)₂, C(O)NHOH, C(O)NHOR¹², C(O)NHSO₂R¹², C(O)NR¹²SO₂R¹², SO₂NH₂,SO₂NHR¹², SO₂N(R¹²)₂, C(O)H, C(O)OH, C(N)NH₂, C(N)NHR¹², C(N)N(R¹²)₂,CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R⁹ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of R¹³, OR¹³, SR¹³, S(O)R¹³, SO₂R¹³, C(O)R¹³,CO(O)R¹³, OC(O)R¹³, OC(O)OR¹³, NH₂, NHR¹³, N(R¹³)₂, NHC(O)R¹³,NR¹³C(O)R¹³, NHS(O)₂R¹³, NR¹³S(O)₂R¹³, NHC(O)OR¹³, NR¹³C(O)OR¹³,NHC(O)NH₂, NHC(O)NHR¹³, NHC(O)N(R¹³)₂, NR¹³C(O)NHR¹³, NR¹³C(O)N(R¹³)₂,C(O)NH₂, C(O)NHR¹³, C(O)N(R¹³)₂, C(O)NHOH, C(O)NHOR¹³, C(O)NHSO₂R¹³,C(O)NR¹³SO₂R¹³, SO₂NH₂, SO₂NHR¹³, SO₂N(R¹³)₂, C(O)H, C(O)OH, C(N)NH₂,C(N)NHR¹³, C(N)N(R¹³)₂, CNOH, CNOCH₃, OH, CN, N₃, NO₂, F, Cl, Br and I;R¹⁰ at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, C₁₋₆ haloalkyl,and C₁₋₆ hydroxyalkyl; R¹¹, at each occurrence, is independentlyselected from the group consisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆alkynyl, aryl, heterocycloalkyl, heterocycloalkenyl, heteroaryl,cycloalkyl, and cycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, andC₂₋₆ alkynyl represented by R¹¹ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of C₁₋₆ alkoxy, aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, cycloalkenyl, NH₂, C(O)H,C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I; wherein the aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl represented by R¹¹ are each independently optionallysubstituted with one or more substituents independently selected fromthe group consisting of NH₂, C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Brand I; R¹², at each occurrence, is independently selected from the groupconsisting of C₁₋₆ alkyl, C₂₋₆ alkenyl, C₂₋₆ alkynyl, aryl,heterocycloalkyl, heterocycloalkenyl, heteroaryl, cycloalkyl, andcycloalkenyl; wherein the C₁₋₆ alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynylrepresented by R¹² are each independently optionally substituted withone or more substituents independently selected from the groupconsisting of C₁₋₆ alkoxy, aryl, heterocycloalkyl, heterocycloalkenyl,heteroaryl, cycloalkyl, cycloalkenyl, NH₂, C(O)H, C(O)OH, OH, CN, N₃,NO₂, F, Cl, Br and I; wherein the aryl, heterocycloalkyl,heterocycloalkenyl, heteroaryl, cycloalkyl, and cycloalkenyl representedby R¹² are each independently optionally substituted with one or moresubstituents independently selected from the group consisting of NH₂,C(O)H, C(O)OH, OH, CN, N₃, NO₂, F, Cl, Br and I; and R¹³, at eachoccurrence, is independently selected from the group consisting of C₁₋₆alkyl, C₂₋₆ alkenyl, and C₂₋₆ alkynyl; wherein the C₁₋₆ alkyl, C₂₋₆alkenyl, and C₂₋₆ alkynyl represented by R¹³ are each independentlyoptionally substituted with one or more substituents independentlyselected from the group consisting of alkoxy, NH₂, C(O)H, C(O)OH, OH,CN, N₃, NO₂, F, Cl, Br and I.
 11. The compound of claim 10, or apharmaceutically acceptable salt thereof, selected from the groupconsisting of:2-[(4-fluorobenzyl)(tetrahydro-2H-pyran-4-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(cyclohexylacetyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl)(3-methylbutanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzoyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(3-chlorobenzoyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzoyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl)(methoxyacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(N,N-dimethylglycyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(3,6-dihydropyridin-1(2H)-ylacetyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(4-methylpiperidin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(4-hydroxypiperidin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(4-methylpiperazin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl){[4-(propan-2-yl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(4-formylpiperazin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl)(hexahydropyrrolo[1,2-a]pyrazin-2(1H)-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[{[4-(cyclopropylmethyl)piperazin-1-yl]acetyl}(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[{[4-(2-ethoxyethyl)piperazin-1-yl]acetyl}(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(cyclopropylcarbonyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl){[4-(prop-2-en-1-yl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl){[4-(3-methoxypropyl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[{[3-(dimethylamino)pyrrolidin-1-yl]acetyl}(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl)(morpholin-4-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{(4-fluorobenzyl)[(3-hydroxypiperidin-1-yl)acetyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-fluorobenzyl){[4-(2-hydroxyethyl)piperazin-1-yl]acetyl}amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(1,4-dioxa-7-azaspiro[4.4]non-7-ylacetyl)(4-fluorobenzyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;1-{2-[(4-fluorobenzyl)(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)amino]-2-oxoethyl}pyridinium;2-{[2-(4-fluorophenyl)ethyl](3-methylbutanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[2-(4-cyanophenyl)ethyl](3-methylbutanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[2-(4-cyanophenyl)ethyl](tetrahydro-2H-pyran-4-ylacetyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzyl)(3-methylbutanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzyl)(tetrahydro-2H-pyran-4-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[2-(4-cyanophenyl)ethyl](tetrahydrofuran-3-ylacetyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzyl)(tetrahydrofuran-3-ylacetyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(4-cyanobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N¹-(4-fluorobenzyl)-N¹-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)piperidine-1,3-dicarboxamide;2-{(4-fluorobenzyl)[(3-hydroxyazetidin-1-yl)carbonyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-1,4-dioxa-7-azaspiro[4.4]nonane-7-carboxamide;2-{(4-fluorobenzyl)[(3-methoxypyrrolidin-1-yl)carbonyl]amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-2,6-dimethylmorpholine-4-carboxamide;N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-2,2-dimethylmorpholine-4-carboxamide;N-(4-fluorobenzyl)-N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-1,4-oxazepane-4-carboxamide;2-[(4-fluorobenzoyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(4-methylbenzyl)amino]-1,3-thiazole-5-carboxamide;N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-N-(3-methylbutyl)-1,2-oxazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(2-phenoxypropanoyl)amino]-1,3-thiazole-5-carboxamide;2-{[2-(4-cyanophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(pyrimidin-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(2-methoxypyridin-4-yl)methyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(1,3-oxazol-4-ylmethyl)amino]-1,3-thiazole-5-carboxamide;2-{[(5-chloropyridin-2-yl)methyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(4-methylpyridin-3-yl)methyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(6-methoxypyridin-3-yl)methyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(4-methyl-1,3-thiazol-5-yl)methyl]amino}-1,3-thiazole-5-carboxamide;2-{[2-(3-hydroxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(pyridin-2-yl)ethyl]amino}-1,3-thiazole-5-carboxamideacetate (1:1);2-{[2-(1,3-benzodioxol-5-yl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamideacetate (1:1);2-{[2-(4-chlorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamideacetate (1:1);2-{[2-(3-fluorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamideacetate (1:1);2-{[2-(4-hydroxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamideacetate (1:1);2-{[2-(3-chlorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamideacetate (1:1);N-[3-(1H-imidazol-1-yl)propyl]-2-{[2-(3-methoxyphenyl)ethyl](3-methoxypropanoyl)amino}-1,3-thiazole-5-carboxamideacetate (1:1);2-{[2-(2-fluorophenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamideacetate (1:1);2-{[2-hydroxy-2-(4-methoxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamideacetate (1:1);N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[1-(pyridin-2-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(1-methyl-1H-pyrazol-4-yl)methyl]amino}-1,3-thiazole-5-carboxamide;2-[(2,6-difluorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(6-methylpyridin-3-yl)methyl]amino}-1,3-thiazole-5-carboxamide;2-[(4-chlorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(5-methylpyrazin-2-yl)methyl]amino}-1,3-thiazole-5-carboxamide;2-[(3-chlorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(5-methylpyridin-2-yl)methyl]amino}-1,3-thiazole-5-carboxamide;2-[(2,5-difluorobenzyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(2-methylbenzyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(3-methylbenzyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(pyridin-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(pyridin-3-ylmethyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methylbutyl)[(2R)-2-phenoxypropanoyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methylbutyl)[(2S)-2-phenoxypropanoyl]amino}-1,3-thiazole-5-carboxamide;N-(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)-5-methyl-N-(3-methylbutyl)-1,2-oxazole-3-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(phenoxyacetyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(3-phenylpropanoyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(2-phenylpropanoyl)amino]-1,3-thiazole-5-carboxamide;2-{[(4-fluorophenyl)acetyl](3-methylbutyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(3-methylbutyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(methoxyacetyl)(3-methylbutyl)amino]-1,3-thiazole-5-carboxamide;2-[(cyclopropylcarbonyl)(3-methylbutyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;(2S)-1-[(5-{[3-(1H-imidazol-1-yl)propyl]carbamoyl}-1,3-thiazol-2-yl)(3-methylbutyl)amino]-1-oxopropan-2-ylacetate;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydro-2H-pyran-4-ylacetyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydrofuran-3-ylcarbonyl)amino]-1,3-thiazole-5-carboxamide;2-{[2-hydroxy-2-(3-methoxyphenyl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(pyrazin-2-ylethyl]amino}-1,3-thiazole-5-carboxamide;2-{[1-(3-hydroxyphenyl)propan-2-yl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydrofuran-2-ylacetyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methylbutyl)(tetrahydrofuran-3-ylacetyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(3-methoxypropanoyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(3-methoxypropyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(tetrahydro-2H-pyran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl)(tetrahydrofuran-2-ylmethyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(propan-2-yloxy)ethyl]amino}-1,3-thiazole-5-carboxamide;2-{[2-(1,3-dioxolan-2-yl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(1,4-dioxan-2-ylmethyl)(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[3-(4-fluorophenyl)propanoyl](2-methoxyethyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(2-methoxyethyl)[3-(pyridin-3-yl)propanoyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(pyridin-3-ylacetyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(naphthalen-2-ylacetyl)amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(2-methoxyethyl)[(4-phenoxyphenyl)acetyl]amino}-1,3-thiazole-5-carboxamide;2-{[(4-cyanophenyl)acetyl](2-methoxyethyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[(4-aminophenyl)acetyl](2-methoxyethyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[{2-[di(prop-2-en-1-yl)amino]ethyl}(3-methoxypropanoyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[3-(diethylamino)propyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[2-(diethylamino)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-(pyrrolidin-1-yl)propyl]amino}-1,3-thiazole-5-carboxamide;2-{[(1-ethyl-5-oxopyrrolidin-3-yl)methyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[(5-oxopyrrolidin-2-yl)methyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-oxo-3-(pyrrolidin-1-yl)propyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-oxo-2-(piperidin-1-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-(2-oxopyrrolidin-1-yl)propyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-(2-oxo-1,3-oxazolidin-3-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-[(3-methoxypropanoyl){2-[(2-methylpropanoyl)amino]ethyl}amino]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[3-(methylamino)-3-oxopropyl]amino}-1,3-thiazole-5-carboxamide;2-{[3-(acetylamino)propyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;N-[3-(1H-imidazol-1-yl)propyl]-2-{(3-methoxypropanoyl)[2-oxo-2-(pyrrolidin-1-yl)ethyl]amino}-1,3-thiazole-5-carboxamide;2-{[(5-chloropyridin-2-yl)methyl](tetrahydro-2H-pyran-4-ylcarbonyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[(5-chloropyridin-2-yl)methyl](tetrahydrofuran-3-ylcarbonyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[2-(5-chloropyridin-2-yl)ethyl](3-methoxypropanoyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-{[2-(5-chloropyridin-2-yl)ethyl](tetrahydrofuran-3-ylcarbonyl)amino}-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;2-[(1,3-benzodioxol-5-ylacetyl)(2-methoxyethyl)amino]-N-[3-(1H-imidazol-1-yl)propyl]-1,3-thiazole-5-carboxamide;andN-[3-(1H-imidazol-1-yl)propyl]-2-[(2-methoxyethyl)(pyridin-2-ylacetyl)amino]-1,3-thiazole-5-carboxamide.